ANTONELLO MAI

Antonello Mai, nato a Roma, ha conseguito la laurea in Farmacia presso la facoltà di Farmacia dell’Università degli Studi di Roma “La Sapienza” con voti 110/110 e lode.
Nel 1990 il dott. Antonello Mai è risultato vincitore di un concorso per Funzionario Tecnico presso il Dipartimento di Studi Farmaceutici dell’Università degli Studi di Roma “La Sapienza”.
Nel giugno 1992 il dott. Antonello Mai ha conseguito il titolo di Dottore di Ricerca in Scienze Farmaceutiche discutendo una tesi dal titolo “Ricerche su nuove benzodiazepine policicliche attive sul Sistema Nervoso Centrale”, relatore il chiar.mo prof. Marino Artico.
Il 28 agosto 1998 con D.M. 6/08/1998 il dott. Antonello Mai è risultato vincitore di un concorso a posti di professore universitario di ruolo II fascia (bandito con DD.MM. 22/12/95 e 29/2/96) per il raggruppamento C07X-Chimica Farmaceutica.
Nel luglio 2010 il prof. Mai è risultato idoneo ad un concorso per professore universitario di ruolo I fascia per il settore CHIM/08, Chimica Farmaceutica, bandito da Sapienza Università di Roma.
Il 1° dicembre 2011 il Prof. A. Mai ha preso servizio come Prof. Ordinario per il SSD CHIM/08 presso Sapienza Università di Roma.
Dall’a.a. 2011/2012 è titolare dell’insegnamento “Chimica Farmaceutica e Tossicologica 2” e “Chimica Farmaceutica e Tossicologica 3” per il CdL in CTF, facoltà di Farmacia e Medicina.

Editorial Boards: Il prof. Antonello Mai è Chair Editor di “ChemMedChem” (Wiley), Regional Editor delle riviste “Mini Reviews in Medicinal Chemistry” (Bentham) e “Medicinal Chemistry” (Bentham) e Associate Editor di “Clinical Epigenetics” e “Journal of Enzyme Inhibition and Medicinal Chemistry”.

Honors: Il prof. Mai dal 1992 è membro della SCI (Società Chimica Italiana). Dal 2004 to 2009 è stato membro dell’Executive Committee della Divisione di Chimica Farmaceutica della SCI. Dal 2009 al 2014 il prof. Mai è stato membro dello Scientific Committee della European School of Medicinal Chemistry (ESMEC). Nel 2015 è stato membro dell’Executive Committee della European Federation of Medicinal Chemistry (EFMC).
Dal 2012 al 2018, il prof. Mai è stato Coordinatore del Dottorato in Scienze Farmaceutiche, afferente alla Scuola di Dottorato in Biologia e Medicina Molecolare (BEMM), in Sapienza Università di Roma.
Dal 2013 al 2019, il prof. Mai è stato Presidente del Corso di Laurea Magistrale a Ciclo Unico in Chimica e Tecnologia Farmaceutiche, Facoltà di Farmacia e Medicina, Sapienza Università di Roma.
Dal 2014 al 2022, il prof. Mai è stato membro della Commissione Istruttoria per i Dottorati di Ricerca di Sapienza Università di Roma, che assicura la qualità dei Dottorati di Ricerca Sapienza preparandoli ad hoc per l’approvazione da parte dell’ANVUR.
Dal 2015 è Esperto di Sistema per ANVUR.
Dal 2019 è membro del Team Qualità di Sapienza Università di Roma.

L’attività di ricerca del prof. Antonello Mai, espressa in oltre 400 pubblicazioni, 8 brevetti, 6 capitoli di libro ed oltre 500 comunicazioni a congressi, può essere riferita a quattro settori fondamentali: a) progettazione e sintesi di piccole molecole come modulatori di target epigenetici coinvolti nel controllo di trascrizione genica (HDACs, HATs, SIRTs, HMTs, HDMs, DNMT). Potenzialità terapeutiche nel campo dell’oncologia e delle malattie neurodegenerative e muscolari; b) ricerche su sostanze attive sul S.N.C.; c) ricerche su sostanze ad attività antivirale (inibitori specifici della trascrittasi inversa dell’HIV-1); d) ricerche su sostanze ad attività antibatterica, antimicobatterica ed antifungina.

Totale pubblicazioni (fonte: Scopus): 415 (06.05.25)
H-index: 69 (06.05.25)
n. citazioni: 17.348

Ultimi progetti approvati per il finanziamento:
2023 research project: PRIN (from Italian Government) 2022 PNRR, title: “Targeting a professional ROS generator in cancer and inflammation”: role: Responsible of Research Unit, Co-Principal Investigator. 125,000 euro.
2022 research project: Pasteur Institute - Cenci Bolognetti Foundation, two-year (2021-2022) project, title: “Epi-drugs for treatment of parasitic diseases”; role: Principal Investigator (PI). 40,000 euro.
2021 research project: Fondo Integrativo Speciale per la Ricerca (FISR) 2019, title: “Methylome Dysregulation in Cancer: a Synergistic Multidisciplinary Approach for Fighting (MeDyCa); role: Principal Investigator. 673,600 euro.
2017 research project: NIH 2017-2020, title: “Histone Lysine deMethylation: Structures, Inhibitions and Mechanisms (Project 00006104)”; role: co-investigator. $ 107,036.
2016 research project: AIRC 2016-2019, title: “Targeting histone demethylation for cancer therapy: development of new LSD1 inhibitors”; role: Principal Investigator. 286,000 euro.
2015 research project: PRIN (from Italian Government) 2015, title: “Epitargeting of Acute Myeloid Leukemia: a Synergistic Multidisciplinary Approach”; role: Principal Investigator. 81,500 euro.

Lista di pubblicazioni del Prof. ANTONELLO MAI anni 2015-2024

1. Zhou J, Chen Q, Ren R, Yang J, Liu B, Horton JR, Chang C, Li C, Maksoud L, Yang Y, Rotili D, Jain AK, Zhang X, Blumenthal RM, Chen T, Gao Y, Valente S, Mai A, Cheng X. Quinoline-based compounds can inhibit diverse enzymes that act on DNA. Cell Chem Biol. 2024 Oct 14:S2451-9456(24)00403-3. doi: 10.1016/j.chembiol.2024.09.007.
2. Fiorentino F, Fabbrizi E, Mai A, Rotili D. Activation and inhibition of sirtuins: From bench to bedside. Med Res Rev. 2024 Aug 31. doi: 10.1002/med.22076.
3. Cassandri M, Porrazzo A, Pomella S, Noce B, Zwergel C, Aiello FA, Vulcano F, Milazzo L, Camero S, Pajalunga D, Spada M, Manzi V, Gravina GL, Codenotti S, Piccione M, Tomaciello M, Signore M, Barillari G, Marchese C, Fanzani A, De Angelis B, Quintarelli C, Vakoc CR, Chen EY, Megiorni F, Locatelli F, Valente S, Mai A, Rota R, Marampon F. HDAC3 genetic and pharmacologic inhibition radiosensitizes fusion positive rhabdomyosarcoma by promoting DNA double-strand breaks. Cell Death Discov. 2024 Aug 6;10(1):351. doi: 10.1038/s41420-024-02115-y.
4. Spizzichino S, Di Fonzo F, Marabelli C, Tramonti A, Chaves-Sanjuan A, Parroni A, Boumis G, Liberati FR, Paone A, Montemiglio LC, Ardini M, Jakobi AJ, Bharadwaj A, Swuec P, Tartaglia GG, Paiardini A, Contestabile R, Mai A, Rotili D, Fiorentino F, Macone A, Giorgi A, Tria G, Rinaldo S, Bolognesi M, Giardina G, Cutruzzolà F. Structure-based mechanism of riboregulation of the metabolic enzyme SHMT1. Mol Cell. 2024 Jul 25;84(14):2682-2697.e6. doi: 10.1016/j.molcel.2024.06.016.
5. Aventaggiato M, Arcangeli T, Vernucci E, Barreca F, Sansone L, Pellegrini L, Pontemezzo E, Valente S, Fioravanti R, Russo MA, Mai A, Tafani M. Pharmacological Activation of SIRT3 Modulates the Response of Cancer Cells to Acidic pH. Pharmaceuticals (Basel). 2024 Jun 20;17(6):810. doi: 10.3390/ph17060810.
6. Garbo S, D'Andrea D, Colantoni A, Fiorentino F, Mai A, Ramos A, Tartaglia GG, Tancredi A, Tripodi M, Battistelli C. m6A modification inhibits miRNAs' intracellular function, favoring their extracellular export for intercellular communication. Cell Rep. 2024 Jun 25;43(6):114369. doi: 10.1016/j.celrep.2024.114369.
7. Raucci A, Castiello C, Mai A, Zwergel C, Valente S. Heterocycles-Containing HDAC Inhibitors Active in Cancer: An Overview of the Last Fifteen Years. ChemMedChem. 2024 Sep 16;19(18):e202400194. doi: 10.1002/cmdc.202400194.
8. Maure A, Lawarée E, Fiorentino F, Pawlik A, Gona S, Giraud-Gatineau A, Eldridge MJG, Danckaert A, Hardy D, Frigui W, Keck C, Gutierrez C, Neyrolles O, Aulner N, Mai A, Hamon M, Barreiro LB, Brodin P, Brosch R, Rotili D, Tailleux L. A host-directed oxadiazole compound potentiates antituberculosis treatment via zinc poisoning in human macrophages and in a mouse model of infection. PLoS Biol. 2024 Apr 29;22(4):e3002259. doi: 10.1371/journal.pbio.3002259.
9. Fiorentino F, Fabbrizi E, Raucci A, Noce B, Fioravanti R, Valente S, Paolini C, De Maria R, Steinkühler C, Gallinari P, Rotili D, Mai A. Uracil- and Pyridine-Containing HDAC Inhibitors Displayed Cytotoxicity in Colorectal and Glioblastoma Cancer Stem Cells. ChemMedChem. 2024 Jul 2;19(13):e202300655. doi: 10.1002/cmdc.202300655.
10. Trionfetti F, Montaldo C, Caiello I, Bontempi G, Terri M, Tiberi M, Marchant V, Domenici A, Menè P, Cordani M, Zwergel C, Prencipe G, Ruiz-Ortega M, Valente S, Mai A, Tripodi M, Strippoli R. Mechanisms of mesothelial cell response to viral infections: HDAC1-3 inhibition blocks poly(I:C)-induced type I interferon response and modulates the mesenchymal/inflammatory phenotype. Front Cell Infect Microbiol. 2024 Feb 27;14:1308362. doi: 10.3389/fcimb.2024.1308362.
11. Villares M, Lourenço N, Ktorza I, Berthelet J, Panagiotou A, Richard A, Amo A, Koziy Y, Medjkane S, Valente S, Fioravanti R, Pioche-Durieu C, Lignière L, Chevreux G, Mai A, Weitzman JB. Theileria parasites sequester host eIF5A to escape elimination by host-mediated autophagy. Nat Commun. 2024 Mar 12;15(1):2235. doi: 10.1038/s41467-024-45022-7.
12. Viviano M, Cipriano A, Fabbrizi E, Feoli A, Castellano S, Sbardella G, Mai A, Milite C, Rotili D. Successes and challenges in the development of BD1-selective BET inhibitors: a patent review. Expert Opin Ther Pat. 2024 Jul;34(7):529-545. doi: 10.1080/13543776.2024.2327300.
13. Pecci V, Troisi F, Aiello A, De Martino S, Carlino A, Fiorentino V, Ripoli C, Rotili D, Pierconti F, Martini M, Porru M, Pinto F, Mai A, Bassi PF, Grassi C, Gaetano C, Pontecorvi A, Strigari L, Farsetti A, Nanni S. Targeting of H19/cell adhesion molecules circuitry by GSK-J4 epidrug inhibits metastatic progression in prostate cancer. Cancer Cell Int. 2024 Feb 5;24(1):56. doi: 10.1186/s12935-024-03231-6.
14. Lambona C, Zwergel C, Valente S, Mai A. SIRT3 Activation a Promise in Drug Development? New Insights into SIRT3 Biology and Its Implications on the Drug Discovery Process. J Med Chem. 2024 Feb 8;67(3):1662-1689. doi: 10.1021/acs.jmedchem.3c01979.
15. Terri M, Sandoval P, Bontempi G, Montaldo C, Tomero-Sanz H, de Turris V, Trionfetti F, Pascual-Antón L, Clares-Pedrero I, Battistelli C, Valente S, Zwergel C, Mai A, Rosanò L, Del Pozo MÁ, Sánchez-Álvarez M, Cabañas C, Tripodi M, López-Cabrera M, Strippoli R. HDAC1/2 control mesothelium/ovarian cancer adhesive interactions impacting on Talin-1-α5β1-integrin-mediated actin cytoskeleton and extracellular matrix protein remodeling. J Exp Clin Cancer Res. 2024 Jan 23;43(1):27. doi: 10.1186/s13046-023- 02930-8.
16. Pannek M, Alhalabi Z, Tomaselli D, Menna M, Fiorentino F, Robaa D, Weyand M, Puhlmann M, Tomassi S, Barreca F, Tafani M, Zaganjor E, Haigis MC, Sippl W, Rotili D, Mai A, Steegborn C. Specific Inhibitors of Mitochondrial Deacylase Sirtuin 4 Endowed with Cellular Activity. J Med Chem. 2024 Feb 8;67(3):1843-1860. doi: 10.1021/acs.jmedchem.3c01496.
17. Trionfetti F, Alonzi T, Bontempi G, Terri M, Battistelli C, Montaldo C, Repele F, Rotili D, Valente S, Zwergel C, Matusali G, Maggi F, Goletti D, Tripodi M, Mai A, Strippoli R. HDAC1-3 inhibition increases SARS-CoV-2 replication and productive infection in lung mesothelial and epithelial cells. Front Cell Infect Microbiol. 2023 Dec 13;13:1257683. doi: 10.3389/fcimb.2023.1257683.
18. Marchant V, Trionfetti F, Tejedor-Santamaria L, Rayego-Mateos S, Rotili D, Bontempi G, Domenici A, Menè P, Mai A, Martín-Cleary C, Ortiz A, Ramos AM, Strippoli R, Ruiz-Ortega M. BET Protein Inhibitor JQ1 Ameliorates Experimental Peritoneal Damage by Inhibition of Inflammation and Oxidative Stress. Antioxidants (Basel). 2023 Nov 29;12(12):2055. doi: 10.3390/antiox12122055.
19. Cesaro B, Iaiza A, Piscopo F, Tarullo M, Cesari E, Rotili D, Mai A, Diana A, Londero M, Del Giacco L, Masetti R, Di Leone A, Naro C, Masciarelli S, Fontemaggi G, Sette C, Fazi F, Fatica A. Enhancing sensitivity of triple-negative breast cancer to DNA-damaging therapy through chemical inhibition of the m6A methyltransferase METTL3. Cancer Commun (Lond). 2024 Feb;44(2):282-286. doi: 10.1002/cac2.12509.
20. Reis J, Gorgulla C, Massari M, Marchese S, Valente S, Noce B, Basile L, Törner R, Cox H 3rd, Viennet T, Yang MH, Ronan MM, Rees MG, Roth JA, Capasso L, Nebbioso A, Altucci L, Mai A, Arthanari H, Mattevi A. Targeting ROS production through inhibition of NADPH oxidases. Nat Chem Biol. 2023 Dec;19(12):1540-1550. doi: 10.1038/s41589-023-01457-5.
21. Boissavy T, Rotili D, Mouveaux T, Roger E, Aliouat EM, Pierrot C, Valente S, Mai A, Gissot M. Hydroxamate-based compounds are potent inhibitors of Toxoplasma gondii HDAC biological activity. Antimicrob Agents Chemother. 2023 Nov 15;67(11):e0066123. doi: 10.1128/aac.00661-23.
22. Wang J, Luo J, Rotili D, Mai A, Steegborn C, Xu S, Jin ZG. SIRT6 Protects Against Lipopolysaccharide-Induced Inflammation in Human Pulmonary Lung Microvascular Endothelial Cells. Inflammation. 2024 Feb;47(1):323-332. doi: 10.1007/s10753-023-01911-5.
23. Fiorentino F, Carta F, Rotili D, Mai A, Supuran CT. State of the art of carbonic anhydrase activators. Future Med Chem. 2023 Nov;15(22):2025-2028. doi: 10.4155/fmc-2023-0193.
24. Scribani Rossi C, Eckartt K, Scarchilli E, Angeli S, Price-Whelan A, Di Matteo A, Chevreuil M, Raynal B, Arcovito A, Giacon N, Fiorentino F, Rotili D, Mai A, Espinosa-Urgel M, Cutruzzolà F, Dietrich LEP, Paone A, Paiardini A, Rinaldo S. Molecular insights into RmcA-mediated c-di-GMP consumption: Linking redox potential to biofilm morphogenesis in Pseudomonas aeruginosa. Microbiol Res. 2023 Dec;277:127498. doi: 10.1016/j.micres.2023.127498.
25. Barreca F, Aventaggiato M, Vitiello L, Sansone L, Russo MA, Mai A, Valente S, Tafani M. SIRT5 Activation and Inorganic Phosphate Binding Reduce Cancer Cell Vitality by Modulating Autophagy/Mitophagy and ROS. Antioxidants (Basel). 2023 Aug 18;12(8):1635. doi: 10.3390/antiox12081635.
26. Fiorentino F, Mai A, Rotili D. The role of structural biology in the design of sirtuin activators. Curr Opin Struct Biol. 2023 Oct;82:102666. doi: 10.1016/j.sbi.2023.102666.
27. Lambona C, Zwergel C, Fioravanti R, Valente S, Mai A. Histone deacetylase 10: A polyamine deacetylase from the crystal structure to the first inhibitors. Curr Opin Struct Biol. 2023 Oct;82:102668. doi: 10.1016/j.sbi.2023.102668.
28. Zwergel C, Aventaggiato M, Garbo S, Di Bello E, Fassari B, Noce B, Castiello C, Lambona C, Barreca F, Rotili D, Fioravanti R, Schmalz T, Weyand M, Niedermeier A, Tripodi M, Colotti G, Steegborn C, Battistelli C, Tafani M, Valente S, Mai A. Novel 1,4-Dihydropyridines as Specific Binders and Activators of SIRT3 Impair Cell Viability and Clonogenicity and Downregulate Hypoxia-Induced Targets in Cancer Cells. J Med Chem. 2023 Jul 27;66(14):9622-9641. doi: 10.1021/acs.jmedchem.3c00337.
29. Fiorentino F, Sementilli S, Menna M, Turrisi F, Tomassi S, Pellegrini FR, Iuzzolino A, D'Acunzo F, Feoli A, Wapenaar H, Taraglio S, Fraschetti C, Del Bufalo D, Sbardella G, Dekker FJ, Paiardini A, Trisciuoglio D, Mai A, Rotili D. First-in-Class Selective Inhibitors of the Lysine Acetyltransferase KAT8. J Med Chem. 2023 May 25;66(10):6591-6616. doi: 10.1021/acs.jmedchem.2c01937.
30. Zhou J, Deng Y, Iyamu ID, Horton JR, Yu D, Hajian T, Vedadi M, Rotili D, Mai A, Blumenthal RM, Zhang X, Huang R, Cheng X. Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and a Clostridioides difficile-Specific DNA Adenine Methyltransferase. ACS Chem Biol. 2023 Apr 21;18(4):734-745. doi: 10.1021/acschembio.3c00035.
31. Fabbrizi E, Fiorentino F, Carafa V, Altucci L, Mai A, Rotili D. Emerging Roles of SIRT5 in Metabolism, Cancer, and SARS-CoV-2 Infection. Cells. 2023 Mar 9;12(6):852. doi: 10.3390/cells12060852.
32. Fiorentino F, Nocentini A, Rotili D, Supuran CT, Mai A. Antihistamines, phenothiazine-based antipsychotics, and tricyclic antidepressants potently activate pharmacologically relevant human carbonic anhydrase isoforms II and VII. J Enzyme Inhib Med Chem. 2023 Dec;38(1):2188147. doi: 10.1080/14756366.2023.2188147.
33. Aventaggiato M, Barreca F, Vitiello L, Vespa S, Valente S, Rotili D, Mai A, Lotti LV, Sansone L, Russo MA, Bizzarri M, Ferretti E, Tafani M. Role of SIRT3 in Microgravity Response: A New Player in Muscle Tissue Recovery. Cells. 2023 Feb 22;12(5):691. doi: 10.3390/cells12050691.
34. Fiorentino F, Rotili D, Mai A. Native mass spectrometry-directed drug discovery: Recent advances in investigating protein function and modulation. Drug Discov Today. 2023 Mar 4;28(5):103548. doi: 10.1016/j.drudis.2023.103548.
35. Noce B, Di Bello E, Fioravanti R, Mai A. LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials. Front Pharmacol. 2023 Feb 2;14:1120911. doi: 10.3389/fphar.2023.1120911.
36. Fiorentino F, Menna M, Rotili D, Valente S, Mai A. METTL3 from Target Validation to the First Small-Molecule Inhibitors: A Medicinal Chemistry Journey. J Med Chem. 2023 Jan 24. doi: 10.1021/acs.jmedchem.2c01601. PMID: 36370994.
37. Negri A, Marozzi M, Trisciuoglio D, Rotili D, Mai A, Rizzi F. Simultaneous administration of EZH2 and BET inhibitors inhibits proliferation and clonogenic ability of metastatic prostate cancer cells. J Enzyme Inhib Med Chem. 2023 Dec;38(1):2163242. doi: 10.1080/14756366.2022.2163242.
38. Zhou J, Horton JR, Menna M, Fiorentino F, Ren R, Yu D, Hajian T, Vedadi M, Mazzoccanti G, Ciogli A, Weinhold E, Hüben M, Blumenthal RM, Zhang X, Mai A, Rotili D, Cheng X. Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile-Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence. J Med Chem. 2023 Jan 12;66(1):934-950. doi: 10.1021/acs.jmedchem.2c01789.
39. Di Bello E, Sian V, Bontempi G, Zwergel C, Fioravanti R, Noce B, Castiello C, Tomassi S, Corinti D, Passeri D, Pellicciari R, Mercurio C, Varasi M, Altucci L, Tripodi M, Strippoli R, Nebbioso A, Valente S, Mai A. Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells. Eur J Med Chem. 2023 Feb 5;247:115022. doi: 10.1016/j.ejmech.2022.115022.
40. Orekhova A, De Angelis M, Cacciotti A, Reverberi M, Rotili D, Giorgi A, Protto V, Bonincontro G, Fiorentino F, Zgoda V, Mai A, Palamara AT, Simonetti G. Modulation of Virulence-Associated Traits in Aspergillus fumigatus by BET Inhibitor JQ1. Microorganisms. 2022 Nov 18;10(11):2292. doi: 10.3390/microorganisms10112292.
41. Zwergel C, Fioravanti R, Mai A. PD-L1 small-molecule modulators: A new hope in epigenetic-based multidrug cancer therapy? Drug Discov Today. 2023 Feb;28(2):103435. doi: 10.1016/j.drudis.2022.103435.
42. Bontempi G, Terri M, Garbo S, Montaldo C, Mariotti D, Bordoni V, Valente S, Zwergel C, Mai A, Marchetti A, Domenici A, Menè P, Battistelli C, Tripodi M, Strippoli R. Restoration of WT1/miR-769-5p axis by HDAC1 inhibition promotes MMT reversal in mesenchymal-like mesothelial cells. Cell Death Dis. 2022 Nov 17;13(11):965. doi: 10.1038/s41419-022-05398-0.
43. Noce B, Di Bello E, Zwergel C, Fioravanti R, Valente S, Rotili D, Masotti A, Ansari MSZ, Trisciuoglio D, Chakrabarti A, Romier C, Robaa D, Sippl W, Jung M, Häberli C, Keiser J, Mai A. Chemically Diverse S. mansoni HDAC8 Inhibitors Reduced Viability in Worm Larval and Adult Stages. ChemMedChem. 2022 Oct 17. doi: 10.1002/cmdc.202200510.
44. Suenkel B, Valente S, Zwergel C, Weiss S, Di Bello E, Fioravanti R, Aventaggiato M, Amorim JA, Garg N, Kumar S, Lombard DB, Hu T, Singh PK, Tafani M, Palmeira CM, Sinclair D, Mai A, Steegborn C. Potent and Specific Activators for Mitochondrial Sirtuins Sirt3 and Sirt5. J Med Chem. 2022, 65(20),14015-14031. doi: 10.1021/acs.jmedchem.2c01215.
45. Ansari MSZ, Stagni V, Iuzzolino A, Rotili D, Mai A, Del Bufalo D, Lavia P, Degrassi F, Trisciuoglio D. Pharmacological targeting of CBP/p300 drives a redox/autophagy axis leading to senescence-induced growth arrest in non-small cell lung cancer cells. Cancer Gene Ther. 2022 Sep 18. doi: 10.1038/s41417-022-00524-8.
46. Chianese U, Papulino C, Passaro E, Evers TM, Babaei M, Toraldo A, De Marchi T, Niméus E, Carafa V, Nicoletti MM, Del Gaudio N, Iaccarino N, Randazzo A, Rotili D, Mai A, Cappabianca S, Mashaghi A, Ciardiello F, Altucci L, Benedetti R. Histone lysine demethylase inhibition reprograms prostate cancer metabolism and mechanics. Mol Metab. 2022, 64:101561. doi: 10.1016/j.molmet.2022.101561.
47. Fiorentino F, Castiello C, Mai A, Rotili D. Therapeutic Potential and Activity Modulation of the Protein Lysine Deacylase Sirtuin 5. J Med Chem. 2022, 65(14):9580-9606. doi: 10.1021/acs.jmedchem.2c00687.
48. Di Bello E, Noce B, Fioravanti R, Zwergel C, Valente S, Rotili D, Fianco G, Trisciuoglio D, Mourão MM, Sales P Jr, Lamotte S, Prina E, Späth GF, Häberli C, Keiser J, Mai A. Effects of Structurally Different HDAC Inhibitors against Trypanosoma cruzi, Leishmania, and Schistosoma mansoni. ACS Infect Dis. 2022, 8(7):1356-1366. doi: 10.1021/acsinfecdis.2c00232.
49. Cristalli C, Manara MC, Valente S, Pellegrini E, Bavelloni A, De Feo A, Blalock W, Di Bello E, Piñeyro D, Merkel A, Esteller M, Tirado OM, Mai A, Scotlandi K. Novel Targeting of DNA Methyltransferase Activity Inhibits Ewing Sarcoma Cell Proliferation and Enhances Tumor Cell Sensitivity to DNA Damaging Drugs by Activating the DNA Damage Response. Front Endocrinol (Lausanne). 2022, 13:876602. doi: 10.3389/fendo.2022.876602.
50. Fiorentino F, Mautone N, Menna M, D'Acunzo F, Mai A, Rotili D. Sirtuin modulators: past, present, and future perspectives. Future Med Chem. 2022, 14(12):915-939. doi: 10.4155/fmc-2022-0031.
51. Menna M, Fiorentino F, Marrocco B, Lucidi A, Tomassi S, Cilli D, Romanenghi M, Cassandri M, Pomella S, Pezzella M, Del Bufalo D, Zeya Ansari MS, Tomašević N, Mladenović M, Viviano M, Sbardella G, Rota R, Trisciuoglio D, Minucci S, Mattevi A, Rotili D, Mai A. Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models. Eur J Med Chem. 2022, 237:114410. doi: 10.1016/j.ejmech.2022.114410. PMID: 35525212.Taurone S, De Ponte C, Rotili D, De Santis E, Mai A, Fiorentino F, Scarpa S, Artico M, Micera A. Biochemical Functions and Clinical Characterizations of the Sirtuins in Diabetes-Induced Retinal Pathologies. Int J Mol Sci. 2022 Apr 6;23(7):4048. doi: 10.3390/ijms23074048.
2. Consalvi S, Tucciarone L, Macrì E, De Bardi M, Picozza M, Salvatori I, Renzini A, Valente S, Mai A, Moresi V, Puri PL. Determinants of epigenetic resistance to HDAC inhibitors in dystrophic fibro-adipogenic progenitors. EMBO Rep. 2022 Apr 4:e54721. doi: 10.15252/embr.202254721
3. Fioravanti R, Rodriguez V, Caroli J, Chianese U, Benedetti R, Di Bello E, Noce B, Zwergel C, Corinti D, Viña D, Altucci L, Mattevi A, Valente S, Mai A. Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity. J Enzyme Inhib Med Chem. 2022 Dec;37(1):973-985. doi: 10.1080/14756366.2022.2052869.
4. Valentini E, D'Aguanno S, Di Martile M, Montesano C, Ferraresi V, Patsilinakos A, Sabatino M, Antonini L, Chiacchiarini M, Valente S, Mai A, Colotti G, Ragno R, Trisciuoglio D, Del Bufalo D. Targeting the anti-apoptotic Bcl-2 family proteins: machine learning virtual screening and biological evaluation of new small molecules. Theranostics. 2022 Feb 28;12(5):2427-2444. doi: 10.7150/thno.64233.
5. Morroni J, Schirone L, Valenti V, Zwergel C, Riera CS, Valente S, Vecchio D, Schiavon S, Ragno R, Mai A, Sciarretta S, Lozanoska-Ochser B, Bouchè M. Inhibition of PKCθ Improves Dystrophic Heart Phenotype and Function in a Novel Model of DMD Cardiomyopathy. Int J Mol Sci. 2022 Feb 18;23(4):2256. doi: 10.3390/ijms23042256.
6. Siciliano G, Di Paolo V, Rotili D, Migale R, Pedini F, Casella M, Camerini S, Dalzoppo D, Henderson R, Huijs T, Dechering KJ, Mai A, Caccuri AM, Lalle M, Quintieri L, Alano P. The Nitrobenzoxadiazole Derivative NBDHEX Behaves as Plasmodium falciparum Gametocyte Selective Inhibitor with Malaria Parasite Transmission Blocking Activity. Pharmaceuticals (Basel). 2022 Jan 29;15(2):168. doi: 10.3390/ph15020168.
7. Renzini A, Marroncelli N, Cavioli G, Di Francescantonio S, Forcina L, Lambridis A, Di Giorgio E, Valente S, Mai A, Brancolini C, Giampietri C, Magenta A, De Santa F, Adamo S, Coletti D, Moresi V. Cytoplasmic HDAC4 regulates the membrane repair mechanism in Duchenne muscular dystrophy. J Cachexia Sarcopenia Muscle. 2022 Apr;13(2):1339-1359. doi: 10.1002/jcsm.12891.
8. Minisini M, Di Giorgio E, Kerschbamer E, Dalla E, Faggiani M, Franforte E, Meyer-Almes FJ, Ragno R, Antonini L, Mai A, Fiorentino F, Rotili D, Chinellato M, Perin S, Cendron L, Weichenberger CX, Angelini A, Brancolini C. Transcriptomic and genomic studies classify NKL54 as a histone deacetylase inhibitor with indirect influence on MEF2-dependent transcription. Nucleic Acids Res. 2022 Mar 21;50(5):2566-2586. doi: 10.1093/nar/gkac081.
9. Mouveaux T, Rotili D, Boissavy T, Roger E, Pierrot C, Mai A, Gissot M. A potent HDAC inhibitor blocks Toxoplasma gondii tachyzoite growth and profoundly disrupts parasite gene expression. Int J Antimicrob Agents. 2022 Mar;59(3):106526. doi: 10.1016/j.ijantimicag.2022.106526.
10. Riccardi E, Blasi E, Zwergel C, Mai A, Morena M, Campolongo P. Sex-dependent Effects of the Drugs of Abuse Amphetamine and the Smart Drug 3,4-Methylenedioxypyrovalerone on Fear Memory Generalization in Rats. Neuroscience. 2021 Dec 27:S0306-4522(21)00651-5. doi: 10.1016/j.neuroscience.2021.12.027.
11. Nowak RP, Tumber A, Hendrix E, Ansari MSZ, Sabatino M, Antonini L, Andrijes R, Salah E, Mautone N, Pellegrini FR, Simelis K, Kawamura A, Johansson C, Passeri D, Pellicciari R, Ciogli A, Del Bufalo D, Ragno R, Coleman ML, Trisciuoglio D, Mai A, Oppermann U, Schofield CJ, Rotili D. First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53. J Med Chem. 2021 Dec 9;64(23):17031-17050. doi: 10.1021/acs.jmedchem.1c00605.
12. Fiorentino F, Rotili D, Mai A, Bolla JR, Robinson CV. Mass spectrometry enables the discovery of inhibitors of an LPS transport assembly via disruption of protein-protein interactions. Chem Commun (Camb). 2021 Oct 14;57(82):10747-10750. doi: 10.1039/d1cc04186j.
13. Fiorentino F, De Angelis M, Menna M, Rovere A, Caccuri AM, D'Acunzo F, Palamara AT, Nencioni L, Rotili D, Mai A. Anti-influenza A virus activity and structure-activity relationship of a series of nitrobenzoxadiazole derivatives. J Enzyme Inhib Med Chem. 2021 Dec;36(1):2128-2138. doi: 10.1080/14756366.2021.1982932.
14. Tomassi S, Romanelli A, Zwergel C, Valente S, Mai A. Polycomb Repressive Complex 2 Modulation through the Development of EZH2-EED Interaction Inhibitors and EED Binders. J Med Chem. 2021 Aug 26;64(16):11774-11797. doi: 10.1021/acs.jmedchem.1c00226.
15. Mormino A, Cocozza G, Fontemaggi G, Valente S, Esposito V, Santoro A, Bernardini G, Santoni A, Fazi F, Mai A, Limatola C, Garofalo S. Histone-deacetylase 8 drives the immune response and the growth of glioma. Glia. 2021 Nov;69(11):2682-2698. doi: 10.1002/glia.24065.
16. Hu T, Shukla SK, Vernucci E, He C, Wang D, King RJ, Jha K, Siddhanta K, Mullen NJ, Attri KS, Murthy D, Chaika NV, Thakur R, Mulder SE, Pacheco CG, Fu X, High RR, Yu F, Lazenby A, Steegborn C, Lan P, Mehla K, Rotili D, Chaudhary S, Valente S, Tafani M, Mai A, Auwerx J, Verdin E, Tuveson D, Singh PK. Metabolic Rewiring by Loss of Sirt5 Promotes Kras-Induced Pancreatic Cancer Progression. Gastroenterology. 2021 Nov;161(5):1584-1600. doi: 10.1053/j.gastro.2021.06.045.
17. Fiorentino F, Mai A, Rotili D. Emerging Therapeutic Potential of SIRT6 Modulators. J Med Chem. 2021 Jul 22;64(14):9732-9758. doi: 10.1021/acs.jmedchem.1c00601.
18. Molinari F, Feraco A, Mirabilii S, Saladini S, Sansone L, Vernucci E, Tomaselli G, Marzolla V, Rotili D, Russo MA, Ricciardi MR, Tafuri A, Mai A, Caprio M, Tafani M, Armani A. SIRT5 Inhibition Induces Brown Fat-Like Phenotype in 3T3-L1 Preadipocytes. Cells. 2021 May 7;10(5):1126. doi: 10.3390/cells10051126.
19. Fiorentino F, Carafa V, Favale G, Altucci L, Mai A, Rotili D. The Two-Faced Role of SIRT6 in Cancer. Cancers (Basel). 2021 Mar 8;13(5):1156. doi: 10.3390/cancers13051156.
20. Colucci P, Santori A, Romanelli L, Zwergel C, Mai A, Scaccianoce S, Campolongo P. Amphetamine Modulation of Long-Term Object Recognition Memory in Rats: Influence of Stress. Front Pharmacol. 2021 Feb 24;12:644521. doi: 10.3389/fphar.2021.644521.
21. Benedetti R, Papulino C, Sgueglia G, Chianese U, De Marchi T, Iovino F, Rotili D, Mai A, Niméus E, Dell' Aversana C, Altucci L. Regulatory Interplay between miR-181a-5p and Estrogen Receptor Signaling Cascade in Breast Cancer. Cancers (Basel). 2021 Feb 1;13(3):543. doi: 10.3390/cancers13030543.
22. Zwergel C, Di Bello E, Fioravanti R, Conte M, Nebbioso A, Mazzone R, Brosch G, Mercurio C, Varasi M, Altucci L, Valente S, Mai A. Novel Pyridine-Based Hydroxamates and 2'-Aminoanilides as Histone Deacetylase Inhibitors: Biochemical Profile and Anticancer Activity. ChemMedChem. 2021 Mar 18;16(6):989-999. doi: 10.1002/cmdc.202000854.
23. Miele E, Po A, Mastronuzzi A, Carai A, Besharat ZM, Pediconi N, Abballe L, Catanzaro G, Sabato C, De Smaele E, Canettieri G, Di Marcotullio L, Vacca A, Mai A, Levrero M, Pfister SM, Kool M, Giangaspero F, Locatelli F, Ferretti E. Downregulation of miR-326 and its host gene β-arrestin1 induces pro survival activity of E2F1 and promotes medulloblastoma growth. Mol Oncol. 2021 Feb;15(2):523-542. doi: 10.1002/1878-0261.12800.
24. Cassandri M, Fioravanti R, Pomella S, Valente S, Rotili D, Del Baldo G, De Angelis B, Rota R, Mai A. CDK9 as a Valuable Target in Cancer: From Natural Compounds Inhibitors to Current Treatment in Pediatric Soft Tissue Sarcomas. Front Pharmacol. 2020 Aug 13;11:1230. doi: 10.3389/fphar.2020.01230.
25. Fiorentino F, Mai A, Rotili D. Lysine Acetyltransferase Inhibitors From Natural Sources. Front Pharmacol. 2020 Aug 12;11:1243. doi: 10.3389/fphar.2020.01243.
26. Tomaselli D, Mautone N, Mai A, Rotili D. Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs). Eur J Med Chem. 2020 Dec 1;207:112750. doi: 10.1016/j.ejmech.2020.112750.
27. Fioravanti R, Tomassi S, Di Bello E, Romanelli A, Plateroti AM, Benedetti R, Conte M, Novellino E, Altucci L, Valente S, Mai A. Properly Substituted Cyclic Bis-(2-bromobenzylidene) Compounds Behaved as Dual p300/CARM1 Inhibitors and Induced Apoptosis in Cancer Cells. Molecules. 2020 Jul 8;25(14):E3122. doi: 10.3390/molecules25143122.
28. Di Bello E, Zwergel C, Mai A, Valente S. The Innovative Potential of Statins in Cancer: New Targets for New Therapies. Front Chem. 2020 Jun 18;8:516. doi: 10.3389/fchem.2020.00516.
29. Fioravanti R, Mautone N, Rovere A, Rotili D, Mai A. Targeting histone acetylation/deacetylation in parasites: an update (2017-2020). Curr Opin Chem Biol. 2020 Jun 29;57:65-74. doi: 10.1016/j.cbpa.2020.05.008.
30. Coutinho Carneiro V, de Abreu da Silva IC, Amaral MS, Pereira ASA, Silveira GO, Pires DDS, Verjovski-Almeida S, Dekker FJ, Rotili D, Mai A, Lopes-Torres EJ, Robaa D, Sippl W, Pierce RJ, Borrello MT, Ganesan A, Lancelot J, Thiengo S, Fernandez MA, Vicentino ARR, Mourão MM, Coelho FS, Fantappié MR. Pharmacological inhibition of lysine-specific demethylase 1 (LSD1) induces global transcriptional deregulation and ultrastructural alterations that impair viability in Schistosoma mansoni. PLoS Negl Trop Dis. 2020 Jul 1;14(7):e0008332. doi: 10.1371/journal.pntd.0008332.
31. Carafa V, Russo R, Della Torre L, Cuomo F, Dell'Aversana C, Sarno F, Sgueglia G, Di Donato M, Rotili D, Mai A, Nebbioso A, Cobellis G, Chambery A, Altucci L. The Pan-Sirtuin Inhibitor MC2494 Regulates Mitochondrial Function in a Leukemia Cell Line. Front Oncol. 2020 May 21;10:820. doi: 10.3389/fonc.2020.00820.
32. Schiavi S, Melancia F, Carbone E, Buzzelli V, Manduca A, Peinado PJ, Zwergel C, Mai A, Campolongo P, Vanderschuren LJMJ, Trezza V. Detrimental effects of the 'bath salt' methylenedioxypyrovalerone on social play behavior in male rats. Neuropsychopharmacology. 2020 Nov;45(12):2012-2019. doi: 10.1038/s41386-020-0729-5.
33. Iacovino LG, Reis J, Mai A, Binda C, Mattevi A. Diphenylene Iodonium Is a Noncovalent MAO Inhibitor: A Biochemical and Structural Analysis. ChemMedChem. 2020 Aug 5;15(15):1394-1397. doi: 10.1002/cmdc.202000264.
34. Matutino Bastos T, Botelho Pereira Soares M, Haddad Franco C, Alcântara L, Antonini L, Sabatino M, Mautone N, Holanda Freitas-Junior L, Moraes CB, Ragno R, Rotili D, Schenkman S, Mai A, Silvio Moretti N. Identification of Inhibitors to Trypanosoma cruzi Sirtuins Based on Compounds Developed to Human Enzymes. Int J Mol Sci. 2020 May 22;21(10):3659. doi: 10.3390/ijms21103659.
35. Tomaselli D, Steegborn C, Mai A, Rotili D. Sirt4: A Multifaceted Enzyme at the Crossroads of Mitochondrial Metabolism and Cancer. Front Oncol. 2020 Apr 15;10:474. doi: 10.3389/fonc.2020.00474.
36. Ravasio R, Ceccacci E, Nicosia L, Hosseini A, Rossi PL, Barozzi I, Fornasari L, Zuffo RD, Valente S, Fioravanti R, Mercurio C, Varasi M, Mattevi A, Mai A, Pavesi G, Bonaldi T, Minucci S. Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoic acid-induced differentiation. Sci Adv. 2020 Apr 8;6(15):eaax2746. doi: 10.1126/sciadv.aax2746.
37. Caroselli S, Zwergel C, Pirolli A, Sabatino M, Xu Z, Kirsch G, Mai A, Colotti G, Altieri F, Canipari R, Valente S, Ragno R. Discovery of the First Human Arylsulfatase A Reversible Inhibitor Impairing Mouse Oocyte Fertilization. ACS Chem Biol. 2020 Jun 19;15(6):1349-1357. doi: 10.1021/acschembio.9b00999.
38. Mautone N, Zwergel C, Mai A, Rotili D. Sirtuin modulators: where are we now? A review of patents from 2015 to 2019. Expert Opin Ther Pat. 2020 Jun;30(6):389-407. doi: 10.1080/13543776.2020.1749264.
39. Romanelli A, Stazi G, Fioravanti R, Zwergel C, Di Bello E, Pomella S, Perrone C, Battistelli C, Strippoli R, Tripodi M, del Bufalo D, Rota R, Trisciuoglio D, Mai A, Valente S. Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells. ACS Medicinal Chemistry Letters, 2020 Mar 19;11(5):977-983. https://dx.doi.org/10.1021/acsmedchemlett.0c00014
40. Tomassi S, Pfahler J, Mautone N, Rovere A, Esposito C, Passeri D, Pellicciari R, Novellino E, Pannek M, Steegborn C, Paiardini A, Mai A, Rotili D. From PARP1 to TNKS2 Inhibition: A Structure-Based Approach. ACS Medicinal Chemistry Letters 2020, Feb 3;11(5):862-868. https://dx.doi.org/10.1021/acsmedchemlett.9b00654.
41. Reis J, Massari M, Marchese S, Ceccon M, Aalbers FS, Corana F, Valente S, Mai A, Magnani F, Mattevi A. A closer look into NADPH oxidase inhibitors: Validation and insight into their mechanism of action. Redox Biol. 2020 Feb 15;32:101466. doi: 10.1016/j.redox.2020.101466.
42. Zwergel C, Fioravanti R, Stazi G, Sarno F, Battistelli C, Romanelli A, Nebbioso A, Mendes E, Paulo A, Strippoli R, Tripodi M, Pechalrieu D, Arimondo PB, De Luca T, Del Bufalo D, Trisciuoglio D, Altucci L, Valente S, Mai A. Novel Quinoline Compounds Active in Cancer Cells through Coupled DNA Methyltransferase Inhibition and Degradation. Cancers (Basel). 2020 Feb 14;12(2):447. doi: 10.3390/cancers12020447.
43. Fioravanti R, Romanelli A, Mautone N, Di Bello E, Rovere A, Corinti D, Zwergel C, Valente S, Rotili R, Botrugno OA, Dessanti P, Vultaggio S, Vianello P, Cappa A, Binda C, Mattevi A, Minucci S, Mercurio C, Varasi M, Mai A. Tranylcypromine-Based LSD1 Inhibitors: Structure-Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation. ChemMedChem 2020 Apr 3;15(7):643-658, doi: 10.1002/cmdc.201900730.
44. Nobile V, Palumbo F, Lanni S, Ghisio V, Vitali A, Castagnola M, Marzano V, Maulucci G, De Angelis C, De Spirito M, Pacini L, D'Andrea L, Ragno R, Stazi G, Valente S, Mai A, Chiurazzi P, Genuardi M, Neri G, Tabolacci E. Altered Mitochondrial Function in Cells Carrying a Premutation or Unmethylated Full Mutation of the FMR1 Gene. Hum Genet 2020, 139 (2), 227-245. DOI: 10.1007/s00439-019-02104-7.
45. Ferrari A, Longo R, Peri C, Coppi L, Caruso D, Mai A, Mitro N, De Fabiani E, Crestani M. Inhibition of Class I HDACs Imprints Adipogenesis Toward Oxidative and Brown-Like Phenotype. Biochim Biophys Acta Mol Cell Biol Lipids, 2020, 1865 (4), 158594. DOI: 10.1016/j.bbalip.2019.158594.
46. Benedetti R, Dell'Aversana C, De Marchi T, Rotili D, Qing Liu N, Novakovic B, Boccella S, Di Maro S, Cosconati S, Baldi A, Niméus E, Schultz J, Höglund U, Maione S, Papulino C, Chianese U, Iovino F, Federico A, Mai A, Stunnenberg HG, Nebbioso A, Altucci L. Inhibition of Histone Demethylases LSD1 and UTX Regulates ERα Signaling in Breast Cancer. Cancers (Basel) 2019, Dec 16;11(12):2027. DOI: 10.3390/cancers11122027.
47. Colucci P, Mancini GF, Santori A, Zwergel C, Mai A, Trezza V, Roozendaal B, Campolongo P. Amphetamine and the Smart Drug 3,4-Methylenedioxypyrovalerone (MDPV) Induce Generalization of Fear Memory in Rats. Front Mol Neurosci 2019, 12, 292. DOI: 10.3389/fnmol.2019.00292.
48. Stazi G, Taglieri L, Nicolai A, Romanelli A, Fioravanti R, Morrone S, Sabatino M, Ragno R, Taurone S, Nebbioso M, Carletti R, Artico M, Valente S, Scarpa S, Mai A. Dissecting the Role of Novel EZH2 Inhibitors in Primary Glioblastoma Cell Cultures: Effects on Proliferation, Epithelial-Mesenchymal Transition, Migration, and on the Pro-Inflammatory Phenotype. Clin Epigenetics 2019, 11 (1), 173. DOI: 10.1186/s13148-019-0763-5
49. Carafa V, Poziello A, Della Torre L, Giovannelli P, Di Donato M, Safadeh E, Yu Z, Baldi A, Castoria G, Tomaselli D, Mai A, Rotili D, Nebbioso A, Altucci L. Enzymatic and Biological Characterization of Novel Sirtuin Modulators Against Cancer. Int J Mol Sci 2019, 20 (22). DOI: 10.3390/ijms20225654
50. Favia A, Salvatori L, Nanni S, Iwamoto-Stohl LK, Valente S, Mai A, Scagnoli F, Fontanella RA, Totta P, Nasi S, Illi B. The Protein Arginine Methyltransferases 1 and 5 Affect Myc Properties in Glioblastoma Stem Cells. Sci Rep 2019, 9 (1), 15925. DOI: 10.1038/s41598-019-52291-6
51. Monaldi D, Rotili D, Lancelot J, Marek M, Wössner N, Lucidi A, Tomaselli D, Ramos-Morales E, Romier C, Pierce RJ, Mai A, Jung M. Structure-Reactivity Relationships on Substrates and Inhibitors of the Lysine Deacylase Sirtuin 2 From Schistosoma mansoni (Sm Sirt2). J Med Chem 2019, 62 (19), 8733-8759. DOI: 10.1021/acs.jmedchem.9b00638
52. Bacci L, Aiello A, Ripoli C, Loria R, Pugliese D, Pierconti F, Rotili D, Strigari L, Pinto F, Bassi PF, Mai A, Grassi C, Pontecorvi A, Falcioni R, Farsetti A, Nanni S. H19-Dependent Transcriptional Regulation of β3 and β4 Integrins Upon Estrogen and Hypoxia Favors Metastatic Potential in Prostate Cancer. Int J Mol Sci 2019, Aug 17;20(16):4012. DOI: 10.3390/ijms20164012
53. Tomaselli D, Lucidi A, Rotili D, Mai A. Epigenetic Polypharmacology: A New Frontier for Epi-Drug Discovery. Med Res Rev 2020, 40 (1), 190-244. DOI: 10.1002/med.21600.
54. Schlüter A, Aksan B, Fioravanti R, Valente S, Mai A, Mauceri D. Histone Deacetylases Contribute to Excitotoxicity-Triggered Degeneration of Retinal Ganglion Cells In Vivo. Mol Neurobiol 2019, 56 (12), 8018-8034. DOI: 10.1007/s12035-019-01658-x
55. Zwergel C, Schnekenburger M, Sarno F, Battistelli C, Manara MC, Stazi G, Mazzone R, Fioravanti R, Gros C, Ausseil F, Florean C, Nebbioso A, Strippoli R, Ushijima T, Scotlandi K, Tripodi M, Arimondo PB, Altucci L, Diederich M, Mai A, Valente S. Identification of a Novel Quinoline-Based DNA Demethylating Compound Highly Potent in Cancer Cells. Clin Epigenetics 2019, 11 (1), 68. DOI: 10.1186/s13148-019-0663-8
56. Nocentini A, Lucidi A, Perut F, Massa A, Tomaselli D, Gratteri P, Baldini N, Rotili D, Mai A, Supuran CT. α,γ-Diketocarboxylic Acids and Their Esters Act as Carbonic Anhydrase IX and XII Selective Inhibitors. ACS Med Chem Lett 2019, 10 (4), 661-665. DOI: 10.1021/acsmedchemlett.9b00023.
57. Stazi G, Fioravanti R, Mai A, Mattevi A, Valente S. Histone Deacetylases as an Epigenetic Pillar for the Development of Hybrid Inhibitors in Cancer. Curr Opin Chem Biol 2019, 50, 89-100. DOI: 10.1016/j.cbpa.2019.03.002
58. Sirotkin AV, Adamcova E, Rotili D, Mai A, Mlyncek M, Mansour L, Alwasel S, Harrath AH. Comparison of the Effects of Synthetic and Plant-Derived mTOR Regulators on Healthy Human Ovarian Cells. Eur J Pharmacol 2019, 854, 70-78. DOI: 10.1016/j.ejphar.2019.03.048.
59. Mazzone R, Zwergel C, Artico M, Taurone S, Ralli M, Greco A, Mai A.The emerging role of epigenetics in human autoimmune disorders. Clin Epigenetics. 2019 Feb 26;11(1):34. doi: 10.1186/s13148-019-0632-2.
60. Mattioli E, Andrenacci D, Mai A, Valente S, Robijns J, De Vos WH, Capanni C, Lattanzi G. Statins and Histone Deacetylase Inhibitors Affect Lamin A/C - Histone Deacetylase 2 Interaction in Human Cells. Front Cell Dev Biol. 2019 Jan 31;7:6. doi: 10.3389/fcell.2019.00006.
61. Was H, Krol SK, Rotili D, Mai A, Wojtas B, Kaminska B, Maleszewska M. Histone deacetylase inhibitors exert anti-tumor effects on human adherent and stem-like glioma cells. Clin Epigenetics. 2019 Jan 17;11(1):11. doi: 10.1186/s13148-018-0598-5.
62. Atehortua-Martinez LA, Masniere C, Campolongo P, Chasseigneaux S, Callebert J, Zwergel C, Mai A, Laplanche JL, Chen H, Etheve-Quelquejeu M, Mégarbane B, Benturquia N. Acute and chronic neurobehavioral effects of the designer drug and bath salt constituent 3,4-methylenedioxypyrovalerone in the rat. J Psychopharmacol. 2019 Mar;33(3):392-405. doi: 10.1177/0269881118822151.
63. Guida MC, Birse RT, Dall'Agnese A, Toto PC, Diop SB, Mai A, Adams PD, Puri PL, Bodmer R. Intergenerational inheritance of high fat diet-induced cardiac lipotoxicity in Drosophila. Nat Commun. 2019 Jan 14;10(1):193. doi: 10.1038/s41467-018-08128-3.
64. Stazi G, Battistelli C, Piano V, Mazzone R, Marrocco B, Marchese S, Louie SM, Zwergel C, Antonini L, Patsilinakos A, Ragno R, Viviano M, Sbardella G, Ciogli A, Fabrizi G, Cirilli R, Strippoli R, Marchetti A, Tripodi M, Nomura DK, Mattevi A, Mai A, Valente S. Development of alkyl glycerone phosphate synthase inhibitors: Structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells. Eur J Med Chem. 2019 Feb 1;163:722-735. doi: 10.1016/j.ejmech.2018.11.050.
65. Zwergel C, Romanelli A, Stazi G, Besharat ZM, Catanzaro G, Tafani M, Valente S, Mai A. Application of Small Epigenetic Modulators in Pediatric Medulloblastoma. Front Pediatr. 2018 Dec 3;6:370. doi: 10.3389/fped.2018.00370.
66. Nawrozkij M, Forgione M, Yablokov AS, Lucidi A, Tomaselli D, Patsilinakos A, Panella C, Hailu GS, Kirillov IA, Badia R, Riveira Muñoz E, Crespan E, Armijos-Rivera JI, Cirilli R, Ragno R, Este JA, Maga G, Mai A, Rotili D. Effect of α-Methoxy Substitution on the anti-HIV Activity of Dihydropyrimidin-4(3H)-ones. J Med Chem. 2019 Jan 24;62(2):604-621. doi: 10.1021/acs.jmedchem.8b01238.
67. Papale M, Ferretti E, Battaglia G, Bellavia D, Mai A, Tafani M. EZH2, HIF-1, and Their Inhibitors: An Overview on Pediatric Cancers. Front Pediatr. 2018 Nov 19;6:328. doi: 10.3389/fped.2018.00328.
68. Bouchut A, Rotili D, Pierrot C, Valente S, Lafitte S, Schultz J, Hoglund U, Mazzone R, Lucidi A, Fabrizi G, Pechalrieu D, Arimondo PB, Skinner-Adams TS, Chua MJ, Andrews KT, Mai A, Khalife J. Identification of novel quinazoline derivatives as potent antiplasmodial agents. Eur J Med Chem. 2019 Jan 1;161:277-291. doi: 10.1016/j.ejmech.2018.10.041.
69. Fioravanti R, Stazi G, Zwergel C, Valente S, Mai A. Six Years (2012-2018) of Researches on Catalytic EZH2 Inhibitors: The Boom of the 2-Pyridone Compounds. Chem Rec. 2018 Dec;18(12):1818-1832. doi: 10.1002/tcr.201800091.
70. Iachettini S, Trisciuoglio D, Rotili D, Lucidi A, Salvati E, Zizza P, Di Leo L, Del Bufalo D, Ciriolo MR, Leonetti C, Steegborn C, Mai A, Rizzo A, Biroccio A. Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells. Cell Death Dis. 2018 Sep 24;9(10):996. doi: 10.1038/s41419-018-1065-0.
71. Mattioli E, Andrenacci D, Garofalo C, Prencipe S, Scotlandi K, Remondini D, Gentilini D, Di Blasio AM, Valente S, Scarano E, Cicchilitti L, Piaggio G, Mai A, Lattanzi G. Altered modulation of lamin A/C-HDAC2 interaction and p21 expression during oxidative stress response in HGPS. Aging Cell. 2018 Aug 15:e12824. doi: 10.1111/acel.12824.
72. Muñoz-Cobo I, Erburu MM, Zwergel C, Cirilli R, Mai A, Valente S, Puerta E, Tordera RM. Nucleocytoplasmic export of HDAC5 and SIRT2 downregulation: two epigenetic mechanisms by which antidepressants enhance synaptic plasticity markers. Psychopharmacology (Berl). 2018 Aug 8. doi: 10.1007/s00213-018-4975-8.
73. Blanquart C, Linot C, Cartron PF, Tomaselli D, Mai A, Bertrand P. Epigenetic metalloenzymes. Curr Med Chem. 2019; 26(15):2748-2785. doi: 10.2174/0929867325666180706105903.
74. Manara MC, Valente S, Cristalli C, Nicoletti G, Landuzzi L, Zwergel C, Mazzone R, Stazi G, Arimondo PB, Pasello M, Guerzoni C, Picci P, Nanni P, Lollini PL, Mai A, Scotlandi K. A Quinoline-Based DNA Methyltransferase Inhibitor as a Possible Adjuvant in Osteosarcoma Therapy. Mol Cancer Ther. 2018 Sep;17(9):1881-1892. doi: 10.1158/1535-7163.
75. Singh AA, Petraglia F, Nebbioso A, Yi G, Conte M, Valente S, Mandoli A, Scisciola L, Lindeboom R, Kerstens H, Janssen-Megens EM, Pourfarzad F, Habibi E, Berentsen K, Kim B, Logie C, Heath S, Wierenga ATJ, Clarke L, Flicek P, Jansen JH, Kuijpers T, Yaspo ML, Valle VD, Bernard O, Gut I, Vellenga E, Stunnenberg HG, Mai A, Altucci L, Martens JHA. Multi-omics profiling reveals a distinctive epigenome signature for high-risk acute promyelocytic leukemia. Oncotarget. 2018 May 22;9(39):25647-25660. doi: 10.18632/oncotarget.25429.
76. Petraglia F, Singh AA, Carafa V, Nebbioso A, Conte M, Scisciola L, Valente S, Baldi A, Mandoli A, Petrizzi VB, Ingenito C, De Falco S, Cicatiello V, Apicella I, Janssen-Megens EM, Kim B, Yi G, Logie C, Heath S, Ruvo M, Wierenga ATJ, Flicek P, Yaspo ML, Della Valle V, Bernard O, Tomassi S, Novellino E, Feoli A, Sbardella G, Gut I, Vellenga E, Stunnenberg HG, Mai A, Martens JHA, Altucci L. Combined HAT/EZH2 modulation leads to cancer-selective cell death. Oncotarget. 2018 May 22;9(39):25630-25646. doi: 10.18632/oncotarget.25428.
77. Rossi L, Battistelli C, de Turris V, Noce V, Zwergel C, Valente S, Moioli A, Manzione A, Palladino M, Bordoni V, Domenici A, Menè P, Mai A, Tripodi M, Strippoli R. HDAC1 inhibition by MS-275 in mesothelial cells limits cellular invasion and promotes MMT reversal. Sci Rep. 2018 May 31;8(1):8492. doi: 10.1038/s41598-018-26319-2.
78. Zwergel C, Stazi G, Mai A, Valente S. Trends of LSD1 inhibitors in viral infections. Future Med Chem. 2018 May 1;10(10):1133-1136. doi: 10.4155/fmc-2018-0065.
79. Mellini P, Marrocco B, Borovika D, Polletta L, Carnevale I, Saladini S, Stazi G, Zwergel C, Trapencieris P, Ferretti E, Tafani M, Valente S, Mai A. Pyrazole-based inhibitors of enhancer of zeste homologue 2 induce apoptosis and autophagy in cancer cells. Philos Trans R Soc Lond B Biol Sci. 2018 Jun 5;373(1748). pii: 20170150. doi: 10.1098/rstb.2017.0150.
80. Fiorentino F, Mai A, Rotili D. Lysine acetyltransferase inhibitors: structure-activity relationships and potential therapeutic implications. Future Med Chem. 2018 May 1;10(9):1067-1091. doi: 10.4155/fmc-2017-0244.
81. Cocco E, Leo M, Canzonetta C, Di Vito S, Mai A, Rotili D, Di Napoli A, Vecchione A, De Nunzio C, Filetici P, Stoppacciaro A. KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumor aggressiveness and target of KAT inhibitor CPTH2. Clin Epigenetics. 2018 Apr 4;10:44. doi: 10.1186/s13148-018-0473-4.
82. Buonvicino D, Felici R, Ranieri G, Caramelli R, Lapucci A, Cavone L, Muzzi M, Di Pietro L, Bernardini C, Zwergel C, Valente S, Mai A, Chiarugi A. Effects of Class II-Selective Histone Deacetylase Inhibitor on Neuromuscular Function and Disease Progression in SOD1-ALS Mice. Neuroscience. 2018 May 21;379:228-238. doi: 10.1016/j.neuroscience.2018.03.022.
83. Carafa V, Nebbioso A, Cuomo F, Rotili D, Cobellis G, Bontempo P, Baldi A, Spugnini EP, Citro G, Chambery A, Russo R, Ruvo M, Ciana P, Maravigna L, Shaik J, Radaelli E, De Antonellis P, Tarantino D, Pirolli A, Ragno R, Zollo M, Stunnenberg HG, Mai A, Altucci L. RIP1-HAT1-SirT complex identification and targeting in treatment and prevention of cancer. Clin Cancer Res. 2018 Jun 15;24(12):2886-2900. pii: clincanres.3081.2017. doi: 10.1158/1078-0432.CCR-17-3081.
84. Sabatino M, Rotili D, Patsilinakos A, Forgione M, Tomaselli D, Alby F, Arimondo PB, Mai A, Ragno R. Disruptor of telomeric silencing 1-like (DOT1L): disclosing a new class of non-nucleoside inhibitors by means of ligand-based and structure-based approaches. J. Comput. Aided Mol. Des. 2018, Mar;32(3):435-458. doi: 10.1007/s10822-018-0096-z.
85. Kalin JH, Wu M, Gomez AV, Song Y, Das J, Hayward D, Adejola N, Wu M, Panova I, Chung HJ, Kim E, Roberts HJ, Roberts JM, Prusevich P, Jeliazkov JR, Roy Burman SS, Fairall L, Milano C, Eroglu A, Proby CM, Dinkova-Kostova AT, Hancock WW, Gray JJ, Bradner JE, Valente S, Mai A, Anders NM, Rudek MA, Hu Y, Ryu B, Schwabe JWR, Mattevi A, Alani RM, Cole PA. Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors. Nat. Commun. 2018, 9(1), 53. doi: 10.1038/s41467-017-02242-4.
86. Pannek M, Simic Z, Fuszard M, Meleshin M, Rotili D, Mai A, Schutkowski M, Steegborn C. Crystal structures of the mitochondrial deacylase Sirtuin 4 reveal isoform-specific acyl recognition and regulation features. Nat. Commun. 2017, 8(1), 1513. doi: 10.1038/s41467-017-01701-2.
87. Miele E, Valente S, Alfano V, Silvano M, Mellini P, Borovika D, Marrocco B, Po A, Besharat ZM, Catanzaro G, Battaglia G, Abballe L, Zwergel C, Stazi G, Milite C, Castellano S, Tafani M, Trapencieris P, Mai A, Ferretti E. The histone methyltransferase EZH2 as a druggable target in SHH medulloblastoma cancer stem cells. Oncotarget 2017, 8(40), 68557-68570. doi: 10.18632/oncotarget.19782.
88. Lapucci A, Cavone L, Buonvicino D, Felici R, Gerace E, Zwergel C, Valente S, Mai A, Chiarugi A. Effect of Class II HDAC inhibition on glutamate transporter expression and survival in SOD1-ALS mice. Neurosci. Lett. 2017, 656, 120-125. doi: 10.1016/j.neulet.2017.07.033.
89. Mazzone R, Zwergel C, Mai A, Valente S. Epi-drugs in combination with immunotherapy: a new avenue to improve anticancer efficacy. Clin. Epigenetics 2017, 9:59. doi: 10.1186/s13148-017-0358-y.
90. Wapenaar H, van den Bosch T, Leus NGJ, van der Wouden PE, Eleftheriadis N, Hermans J, Hailu GS, Rotili D, Mai A, Dömling A, Bischoff R, Haisma HJ, Dekker FJ. The relevance of Ki calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor. Eur. J. Med. Chem. 2017, 136, 480-486. doi: 10.1016/j.ejmech.2017.05.015.
91. Zwergel C, Czepukojc B, Evain-Bana E, Xu Z, Stazi G, Mori M, Patsilinakos A, Mai A, Botta B, Ragno R, Bagrel D, Kirsch G, Meiser P, Jacob C, Montenarh M, Valente S. Novel coumarin- and quinolinone-based polycycles as cell division cycle 25-A and -C phosphatases inhibitors induce proliferation arrest and apoptosis in cancer cells. Eur. J. Med. Chem. 2017, 134, 316-333. doi: 10.1016/j.ejmech.2017.04.012.
92. Stazi G, Zwergel C, Mai A, Valente S. EZH2 inhibitors: a patent review (2014-2016). Expert Opin. Ther. Pat. 2017, 27, 797-813. doi: 10.1080/13543776.2017.1316976.
93. Madia VN, Benedetti R, Barreca ML, Ngo L, Pescatori L, Messore A, Pupo G, Saccoliti F, Valente S, Mai A, Scipione L, Zheng YG, Tintori C, Botta M, Cecchetti V, Altucci L, Di Santo R, Costi R. Structure-Activity Relationships on Cinnamoyl Derivatives as Inhibitors of p300 Histone Acetyltransferase. ChemMedChem 2017, 12, 1359-1368. doi: 10.1002/cmdc.201700040.
94. Coni S, Mancuso AB, Di Magno L, Sdruscia G, Manni S, Serrao SM, Rotili D, Spiombi E, Bufalieri F, Petroni M, Kusio-Kobialka M, De Smaele E, Ferretti E, Capalbo C, Mai A, Niewiadomski P, Screpanti I, Di Marcotullio L, Canettieri G. Selective targeting of HDAC1/2 elicits anticancer effects through Gli1 acetylation in preclinical models of SHH Medulloblastoma. Sci. Rep. 2017, 7:44079. doi: 10.1038/srep44079.
95. Hailu GS, Robaa D, Forgione M, Sippl W, Rotili D, Mai A. Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. J. Med. Chem. 2017, 60, 4780-4804. doi: 10.1021/acs.jmedchem.6b01595.
96. Moniot S, Forgione M, Lucidi A, Hailu GS, Nebbioso A, Carafa V, Baratta F, Altucci L, Giacché N, Passeri D, Pellicciari R, Mai A, Steegborn C, Rotili D. Development of 1,2,4-Oxadiazoles as Potent and Selective Inhibitors of the Human Deacetylase Sirtuin 2: Structure-Activity Relationship, X-ray Crystal Structure, and Anticancer Activity. J. Med. Chem. 2017, 60, 2344-2360. doi: 10.1021/acs.jmedchem.6b01609.
97. Palanisamy SK, Trisciuoglio D, Zwergel C, Del Bufalo D, Mai A. Metabolite profiling of ascidian Styela plicata using LC-MS with multivariate statistical analysis and their antitumor activity. J. Enzyme Inhib. Med. Chem. 2017, 32, 614-623. doi: 10.1080/14756366.2016.1266344.
98. Božović M, Garzoli S, Sabatino M, Pepi F, Baldisserotto A, Andreotti E, Romagnoli C, Mai A, Manfredini S, Ragno R. Essential Oil Extraction, Chemical Analysis and Anti-Candida Activity of Calamintha nepeta (L.) Savi subsp. glandulosa (Req.) Ball-New Approaches. Molecules 2017, 22. pii: E203. doi: 10.3390/molecules22020203.
99. Fulci C, Rotili D, De Luca A, Stella L, Morozzo Della Rocca B, Forgione M, Di Paolo V, Mai A, Falconi M, Quintieri L, Caccuri AM. A new nitrobenzoxadiazole-based GSTP1-1 inhibitor with a previously unheard of mechanism of action and high stability. J Enzyme Inhib Med Chem 2017, 32, 240-247. doi: 10.1080/14756366.2016.1247059.
100. You W, Rotili D, Li TM, Kambach C, Meleshin M, Schutkowski M, Chua KF, Mai A, Steegborn C. Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules. Angew Chem Int Ed Engl 2017, 56, 1007-1011. doi: 10.1002/anie.201610082.
101. Ourailidou ME, Lenoci A, Zwergel C, Rotili D, Mai A, Dekker FJ. Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity. Bioorg Med Chem 2017, 25, 847-856. doi: 10.1016/j.bmc.2016.11.043.
102. Stunnenberg HG; International Human Epigenome Consortium., Hirst M. The International Human Epigenome Consortium: A Blueprint for Scientific Collaboration and Discovery. Cell 2016, 167, 1145-1149. doi: 10.1016/j.cell.2016.11.007.
103. Ferrari A, Fiorino E, Longo R, Barilla S, Mitro N, Cermenati G, Giudici M, Caruso D, Mai A, Guerrini U, De Fabiani E, Crestani M. Attenuation of diet-induced obesity and induction of white fat browning with a chemical inhibitor of histone deacetylases. Int J Obes (Lond). 2016 Dec 20. doi: 10.1038/ijo.2016.191.
104. Panella S, Marcocci ME, Celestino I, Valente S, Zwergel C, Li Puma DD, Nencioni L, Mai A, Palamara AT, Simonetti G. MC1568 inhibits HDAC6/8 activity and influenza A virus replication in lung epithelial cells: role of Hsp90 acetylation. Future Med Chem. 2016, 8, 2017-2031. doi: 10.4155/fmc-2016-0073.
105. Milite C, Feoli A, Viviano M, Rescigno D, Cianciulli A, Balzano AL, Mai A, Castellano S, Sbardella G. The emerging role of lysine methyltransferase SETD8 in human diseases. Clin Epigenetics. 2016, 8, 102.
106. Speranzini V, Rotili D, Ciossani G, Pilotto S, Marrocco B, Forgione M, Lucidi A, Forneris F, Mehdipour P, Velankar S, Mai A, Mattevi A. Polymyxins and quinazolines are LSD1/KDM1A inhibitors with unusual structural features. Sci Adv. 2016, 2, e1601017. doi: 10.1126/sciadv.1601017.
107. Milite C, Feoli A, Viviano M, Rescigno D, Mai A, Castellano S, Sbardella G. Progress in the Development of Lysine Methyltransferase SETD8 Inhibitors. ChemMedChem 2016, 11, 1680-1685.
108. Carafa V, Rotili D, Forgione M, Cuomo F, Serretiello E, Hailu GS, Jarho E, Lahtela-Kakkonen M, Mai A, Altucci L. Sirtuin functions and modulation: from chemistry to the clinic. Clin Epigenetics. 2016 May 25;8:61.
109. Chano T, Avnet S, Kusuzaki K, Bonuccelli G, Sonveaux P, Rotili D, Mai A, Baldini N. Tumour-specific metabolic adaptation to acidosis is coupled to epigenetic stability in osteosarcoma cells. Am J Cancer Res 2016, 6, 859-875.
110. Stazi G, Zwergel C, Valente S, Mai A. LSD1 inhibitors: a patent review (2010-2015). Expert Opin Ther Pat. 2016, 26, 565-580.
111. Di Martile M, Desideri M, De Luca T, Gabellini C, Buglioni S, Eramo A, Sette G, Milella M, Rotili D, Mai A, Carradori S, Secci D, De Maria R, Del Bufalo D, Trisciuoglio D. Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells. Oncotarget 2016, 7, 11332-11348.
112. Di Liddo R, Valente S, Taurone S, Zwergel C, Marrocco B, Turchetta R, Conconi MT, Scarpa C, Bertalot T, Schrenk S, Mai A, Artico M. Histone deacetylase inhibitors restore IL-10 expression in lipopolysaccharide-induced cell inflammation and reduce IL-1β and IL-6 production in breast silicone implant in C57BL/6J wild-type murine model. Autoimmunity 2016, Jan 20:1-11.
113. van den Bosch T, Boichenko A, Leus NG, Ourailidou ME, Wapenaar H, Rotili D, Mai A, Imhof A, Bischoff R, Haisma HJ, Dekker FJ. The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases. Biochem Pharmacol. 2016, 102, 130-140.
114. Vianello P, Botrugno OA, Cappa A, Dal Zuffo R, Dessanti P, Mai A, Marrocco B, Mattevi A, Meroni G, Minucci S, Stazi G, Thaler F, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C. Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent. J. Med. Chem. 2016, 59, 1501-1517.
115. Valente S, Mellini P, Spallotta F, Carafa V, Nebbioso A, Polletta L, Carnevale I, Saladini S, Trisciuoglio D, Gabellini C, Tardugno M, Zwergel C, Cencioni C, Atlante S, Moniot S, Steegborn C, Budriesi R, Tafani M, Del Bufalo D, Altucci L, Gaetano C, Mai A. 1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells. J. Med. Chem. 2016, 59, 1471-1491.
116. Zwergel C, Valente S, Mai A. DNA Methyltransferases Inhibitors from Natural Sources. Curr. Top. Med. Chem. 2015, 16, 680-696.
117. Wapenaar H, van der Wouden PE, Groves MR, Rotili D, Mai A, Dekker FJ. Enzyme kinetics and inhibition of histone acetyltransferase KAT8. Eur. J. Med. Chem. 2015, 105, 289-296.
118. Erburu M, Muñoz-Cobo I, Domínguez-Andrés J, Beltran E, Suzuki T, Mai A, Valente S, Puerta E, Tordera RM. Chronic stress and antidepressant induced changes in Hdac5 and Sirt2 affect synaptic plasticity. Eur. Neuropsychopharmacol. 2015, 25, 2036-2048.
119. Wang Q, Rosa BA, Nare B, Powell K, Valente S, Rotili D, Mai A, Marshall GR, Mitreva M. Targeting Lysine Deacetylases (KDACs) in Parasites. PLoS Negl Trop Dis. 2015, 9, e0004026.
120. Piano V, Benjamin DI, Valente S, Nenci S, Marrocco B, Mai A, Aliverti A, Nomura DK, Mattevi A. Discovery of Inhibitors for the Ether Lipid-Generating Enzyme AGPS as Anti-Cancer Agents. ACS Chem Biol. 2015, 10, 2589-2597.
121. Di Pompo G, Salerno M, Rotili D, Valente S, Zwergel C, Avnet S, Lattanzi G, Baldini N, Mai A. Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells. J. Med. Chem. 2015, 58, 4073-4079.
122. Zwergel C, Valente S, Jacob C, Mai A. Emerging approaches for histone deacetylase inhibitor drug discovery. Expert Opin. Drug Discov. 2015, 10, 599-613.
123. Graziani G, Artuso S, De Luca A, Muzi A, Rotili D, Scimeca M, Atzori M G, Ceci C, Mai A, Leonetti C, Levati L, Bonanno E, Tentori L, Caccuri A M. A new water soluble MAPK activator exerts antitumor activity in melanoma cells resistant to the BRAF inhibitor vemurafenib. Biochem Pharmacol. 2015, 95, 16-27.
124. Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Monaldi D, Ruoppolo G, Tilset M, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A. Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts. Eur. J. Med. Chem. 2015, 94, 163-174.
125. Pilotto S, Speranzini V, Tortorici M, Durand D, Fish A, Valente S, Forneris F, Mai A, Sixma TK, Vachette P, Mattevi A. Interplay among nucleosomal DNA, histone tails, and corepressor CoREST underlies LSD1-mediated H3 demethylation. Proc. Natl. Acad. Sci. U.S.A. 2015, 112, 2752-2757.
126. Milite C, Feoli A, Sasaki K, La Pietra V, Balzano A L, Marinelli L, Mai A, Novellino E, Castellano S, Tosco A, Sbardella G. A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach. J. Med. Chem. 2015, 58, 2779-2798.
127. Polletta L, Vernucci E, Carnevale I, Arcangeli T, Rotili D, Palmerio S, Steegborn C, Nowak T, Schutkowski M, Pellegrini L, Sansone L, Villanova L, Runci A, Pucci B, Morgante E, Fini M, Mai A, Russo MA, Tafani M. SIRT5 regulation of ammonia-induced autophagy and mitophagy. Autophagy 2015, 11, 253-270.
128. De Luca A, Rotili D, Carpanese D, Lenoci A, Calderan L, Scimeca M, Mai A, Bonanno E, Rosato A, Geroni C, Quintieri L, Caccuri AM. A novel orally active water-soluble inhibitor of human glutathione transferase exerts a potent and selective antitumor activity against human melanoma xenografts. Oncotarget 2015, 6, 4126-4143.
129. Rodriguez V, Valente S, Rovida S, Rotili D, Stazi G, Lucidi A, Ciossani G, Mattevi A, Botrugno O A, Dessanti P, Mercurio C, Vianello P, Minucci S, Varasi M, Mai A. Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells. Med. Chem. Commun. 2015, 6, 665-670.
130. Cencioni C, Spallotta F, Mai A, Martelli F, Farsetti A, Zeiher AM, Gaetano C. Sirtuin function in aging heart and vessels. J. Mol. Cell Cardiol. 2015, 83, 55-61.
131. Gros C, Fleury L, Nahoum V, Faux C, Valente S, Labella D, Cantagrel F, Rilova E, Bouhlel MA, David-Cordonnier M, Dufau I, Ausseil F, Mai A, Mourey L, Lacroix L, Arimondo PB. New Insights on the Mechanism of Quinoline-based DNA Methyltransferase Inhibitors. J. Biol. Chem. 2015, 290, 6293-6302.
132. Rotili D, De Luca A, Tarantino D, Pezzola S, Forgione M, Morozzo Della Rocca B, Falconi M, Mai A, Caccuri A. M. Synthesis and structure-activity relationship of new cytotoxic agents targeting human glutathione-S-transferases. Eur. J. Med. Chem. 2015, 89, 156-171.
133. Mellini P, Valente S, Mai A. Sirtuin modulators: an updated patent review (2012 - 2014). Expert Opin. Ther. Pat. 2015, 25, 5-15.
134. Castellano S, Milite C, Feoli A, Viviano M, Mai A, Novellino E, Tosco A, Sbardella G. Identification of Structural Features of 2-Alkylidene-1,3-Dicarbonyl Derivatives that Induce Inhibition and/or Activation of Histone Acetyltransferases KAT3B/p300 and KAT2B/PCAF. ChemMedChem 2015, 10, 144-157.
135. Valente S, Rodriguez V, Mercurio C, Vianello P, Saponara B, Cirilli R, Ciossani G, Labella D, Marrocco B, Ruoppolo G, Botrugno OA, Dessanti P, Minucci S, Mattevi A, Varasi M, Mai A. Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies. ACS Med Chem Lett. 2015, 6, 173-177.