Discovery and characterization of HIV-1 Inhibitors with innovative mode of action:
-Identification of HIV-1 reverse transcriptase (RT) associated ribonuclease H (RNase H) activity inhibitors
-Identification of HIV-1 Integrase (IN) activity inhibitors
Characterization of human immune innate response evasion by RNA viruses:
-Characterization of Ebola virus VP35 function
-Modulation of host-virus interplay
ResearcherID: G-7327-2014
Scopus Author ID: 54079269600
ORCID ID: 0000-0002-6630-8636
1. Design, synthesis and antiviral evaluation of novel heteroarylcarbothioamide derivatives as dual inhibitors of HIV-1 reverse transcriptase-associated RNase H and RDDP functions. Corona A, Onnis V, Deplano A, Bianco G, Demurtas M, Distinto S, Cheng YC, Alcaro S, Esposito F, Tramontano E. Pathog Dis. 2017 Aug 31;75(6). doi: 10.1093/femspd/ftx078.
2. N-Acylbenzenesulfonamide Dihydro-1,3,4-oxadiazole Hybrids: Seeking Selectivity toward Carbonic Anhydrase Isoforms. Bianco G, Meleddu R, Distinto S, Cottiglia F, Gaspari M, Melis C, Corona A, Angius R, Angeli A, Taverna D, Alcaro S, Leitans J, Kazaks A, Tars K, Supuran CT, Maccioni E. ACS Med Chem Lett. 2017 Jun 21;8(8):792-796. doi: 10.1021/acsmedchemlett.7b00205. eCollection 2017 Aug 10.
3. Multi-target activity of Hemidesmus indicus decoction against innovative HIV-1 drug targets and characterization of Lupeol mode of action.Esposito F, Mandrone M, Vecchio CD, Carli I, Distinto S, Corona A, Lianza M, Piano D, Tacchini M, Maccioni E, Cottiglia F, Saccon E, Poli F, Parolin C, Tramontano E. Pathog Dis. 2017 Jun 20. doi: 10.1093/femspd/ftx065.
4. Uvaria angolensis as a promising source of inhibitors of HIV-1 RT-associated RNA-dependent DNA polymerase and RNase H functions. Ngoutane Mfopa A, Corona A, Eloh K, Tramontano E, Frau A, Boyom FF, Caboni P, Tocco G. Nat Prod Res. 2017 May 25:1-8. doi: 10.1080/14786419.2017.1332615.
5. Chelation Motifs Affecting Metal-dependent Viral Enzymes: N'-acylhydrazone Ligands as Dual Target Inhibitors of HIV-1 Integrase and Reverse Transcriptase Ribonuclease H Domain. Carcelli M, Rogolino D, Gatti A, Pala N, Corona A, Caredda A, Tramontano E, Pannecouque C, Naesens L, Esposito F. Front Microbiol. 2017 Mar 20;8:440. doi: 10.3389/fmicb.2017.00440. eCollection 2017.
6. Natural product-inspired esters and amides of ferulic and caffeic acid as dual inhibitors of HIV-1 reverse transcriptase. Sonar VP, Corona A, Distinto S, Maccioni E, Meleddu R, Fois B, Floris C, Malpure NV, Alcaro S, Tramontano E, Cottiglia F.Eur J Med Chem. 2017 Apr 21;130:248-260. doi: 10.1016/j.ejmech.2017.02.054. Epub 2017 Feb 24.
7. Through scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B. Meleddu R, Distinto S, Cirilli R, Alcaro S, Yanez M, Sanna ML, Corona A, Melis C, Bianco G, Matyus P, Cottiglia F, Maccioni E. J Enzyme Inhib Med Chem. 2017 Dec;32(1):264-270. doi: 10.1080/14756366.2016.1247061.
8. Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding. Martini R, Esposito F, Corona A, Ferrarese R, Ceresola ER, Visconti L, Tintori C, Barbieri A, Calcaterra A, Iovine V, Canducci F, Tramontano E, Botta M.Chembiochem. 2017 Feb 16;18(4):374-377. doi: 10.1002/cbic.201600592. Epub 2017 Jan 18.
9. Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase. Meleddu R, Distinto S, Corona A, Tramontano E, Bianco G, Melis C, Cottiglia F, Maccioni E. J Enzyme Inhib Med Chem. 2017 Dec;32(1):130-136. doi: 10.1080/14756366.2016.1238366. Epub 2016 Oct 21.
10. Sennoside A, derived from the traditional chinese medicine plant Rheum L., is a new dual HIV-1 inhibitor effective on HIV-1 replication. Esposito F, Carli I, Del Vecchio C, Xu L, Corona A, Grandi N, Piano D, Maccioni E, Distinto S, Parolin C, Tramontano E. Phytomedicine. 2016 Nov 15;23(12):1383-1391.
11. New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H. Corona A, di Leva FS, Rigogliuso G, Pescatori L, Madia VN, Subra F, Delelis O, Esposito F, Cadeddu M, Costi R, Cosconati S, Novellino E, di Santo R, Tramontano E Antiviral Res. 2016 Sep 20;134:236-243.
12. Inhibitory Effect of 2,3,5,6-Tetrafluoro-4-[4-(aryl)-1H-1,2,3-triazol-1-yl]benzenesulfonamide Derivatives on HIV Reverse Transcriptase Associated RNase H Activities. Pala N, Esposito F, Rogolino D, Carcelli M, Sanna V, Palomba M, Naesens L, Corona A, Grandi N, Tramontano E, Sechi M. Int J Mol Sci. 2016 Aug 20;17(8). pii: E1371.
13. Biological Activities of Aerial Parts Extracts of Euphorbia characias.Pisano MB, Cosentino S, Viale S, Spanò D, Corona A, Esposito F, Tramontano E, Montoro P, Tuberoso CI, Medda R, Pintus F.Biomed Res Int. 2016;2016:1538703. doi: 10.1155/2016/1538703. Epub 2016 May 24
14. Studies on Cycloheptathiophene-3-carboxamide Derivatives as Allosteric HIV-1 Ribonuclease H Inhibitors. Corona A, Desantis J, Massari S, Distinto S, Masaoka T, Sabatini S, Esposito F, Manfroni G, Maccioni E, Cecchetti V, Pannecouque C, Le Grice SF, Tramontano E, Tabarrini O. ChemMedChem. 2016 Mar 16.
15. Inhibition of HIV-1 Reverse Transcriptase Dimerization by Small Molecules. Tintori C, Corona A, Esposito F, Brai A, Grandi N, Ceresola ER, Clementi M, Canducci F, Tramontano E, Botta M. Chembiochem. 2016 Mar 4. doi: 10.1002/cbic.201500668.
16. Biochemical characterization of a multi-drug resistant HIV-1 subtype AG reverse transcriptase: antagonism of AZT discrimination and excision pathways and sensitivity to RNase H inhibitors. Schneider A, Corona A, Spöring I, Jordan M, Buchholz B, Maccioni E, Di Santo R, Bodem J, Tramontano E, Wöhrl BM. Nucleic Acids Res. 2016 Mar 18;44(5):2310-22
17. Ribonuclease H/DNA Polymerase HIV-1 Reverse Transcriptase Dual Inhibitor: Mechanistic Studies on the Allosteric Mode of Action of Isatin-Based Compound RMNC6. Corona A., Meleddu R., Esposito F., Distinto S., Bianco G., Masaoka T, Maccioni E, Menéndez-Arias L, Alcaro S, Le Grice S.F.J. and Tramontano E. Plos One. 2016
18. A New Vinyl Selenone-Based Domino Approach to Spirocyclopropyl Oxindoles Endowed with Anti-HIV RT Activity. Palomba M, Rossi L, Sancineto L, Tramontano E, Corona A,•BagnoliI L, Santi C,•Pannecouque C,• Tabarrini O, Marini F. Organic & Biomolecular Chemistry 01/2016; DOI:10.1039/C5OB02451J
19. Exploring the thiazole scaffold for the identification of new agents for the treatment of fluconazole resistant Candida. Meleddu R, Distinto S, Corona A, Maccioni E, Arridu A, Melis C, Bianco G, Matyus P, Cottiglia F, Sanna A, De Logu A. Enzyme Inhib Med Chem. 2016 Jan 8:1-6.
20. Antityrosinase activity of Euphorbia characias extracts. Pintus F, Spanò D, Corona A, Medda R. PeerJ. 2015 Oct 13;3:e1305. doi: 10.7717/peerj.1305.
21. 5-Arylaminouracil Derivatives as Potential Dual-Action Agents. Matyugina ES, Novikov MS, Babkov DA, Valuev-Elliston VT, Vanpouille C, Zicari S, Corona A, Tramontano E, Margolis LB, Khandazhinskaya AL, Kochetkov SN.Acta Naturae. 2015 Jul-Sep;7(3):113-5.
22. Kuwanon-L as a New Allosteric HIV-1 Integrase Inhibitor: Molecular Modeling and Biological Evaluation.Esposito F, Tintori C, Martini R, Christ F, Debyser Z, Ferrarese R, Cabiddu G, Corona A, Ceresola ER, Calcaterra A, Iovine V, Botta B, Clementi M, Canducci F, Botta M, Tramontano E. Chembiochem. 2015 Sep 11. doi: 10.1002/cbic.201500385.
23. A Luciferase Reporter Gene Assay to Measure Ebola Virus Viral Protein 35-Associated Inhibition of Double-Stranded RNA-Stimulated, Retinoic Acid-Inducible Gene 1-Mediated Induction of Interferon β.Cannas V, Daino GL, Corona A, Esposito F, Tramontano E.J Infect Dis. 2015 Oct 1;212 Suppl 2:S277-81. doi: 10.1093/infdis/jiv214
24. An Efficient Route to Novel Uracil-Based Drug-Like Molecules BABKOV D.A., CHIZHOV, A.O., KHANDAZHINSKAYA A.L., CORONA A., ESPOSITO F, TRAMONTANO E, SELEY-RADTKE K.L., NOVIKOV M.S.. SYNTHESIS, ISSN: 0039-7881, doi: 10.1055/s-0034-1380405
25. From the traditional Chinese medicine plant Schisandra chinensis new scaffolds effective on HIV-1 reverse transcriptase resistant to non-nucleoside inhibitors. Xu L, Grandi N, Del Vecchio C, Mandas D, Corona A, Piano D, Esposito F, Parolin C, Tramontano E. J Microbiol. 2015 Apr;53(4):288-93. doi: 10.1007/s12275-015-4652-0
26. (3Z)-3-(2-[4-(aryl)-1,3-thiazol-2-yl]hydrazin-1-ylidene)-2,3-dihydro-1H-indol-2-one derivatives as dual inhibitors of HIV-1 reverse transcriptase.Meleddu R, Distinto S, Corona A, Bianco G, Cannas V, Esposito F, Artese A, Alcaro S, Matyus P, Bogdan D, Cottiglia F, Tramontano E, Maccioni E. Eur J Med Chem. 2015 Mar 26;93:452-60. doi: 10.1016/j.ejmech.2015.02.032.
27. Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain. Cuzzucoli Crucitti G, Métifiot M, Pescatori L, Messore A, Madia VN, Pupo G, Saccoliti F, Scipione L, Tortorella S, Esposito F, Corona A, Cadeddu M, Marchand C, Pommier Y, Tramontano E, Costi R, Di Santo R. J Med Chem. 2015 Feb 26;58(4):1915-28. doi: 10.1021/jm501799k.
28. Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by Diketo acid derivatives. Corona A, Di Leva FS, Thierry S, Pescatori L, Cuzzucoli Crucitti G, Subra F, Delelis O, Esposito F, Rigogliuso G, Costi R, Cosconati S, Novellino E, Di Santo R, Tramontano E. Antimicrob Agents Chemother. 2014 Oct;58(10):6101-10. doi: 10.1128/AAC.03605-14.
29. Antiretroviral activity of metal-chelating HIV-1 integrase inhibitors. Carcelli M, Rogolino D, Sechi M, Rispoli G, Fisicaro E, Compari C, Grandi N, Corona A, Tramontano E, Pannecouque C, Naesens L. Eur J Med Chem. 2014 Aug 18;83:594-600. doi: 10.1016/j.ejmech.2014.06.055.
30. Can the ever-promising target HIV reverse transcriptase-associated RNase H become a success story for drug development? Corona A., Esposito F., Tramontano E. Future Virology. (2014) 9(5), 448-445.
31. Design, synthesis, and biological evaluation of 1,3-diarylpropenones as dual inhibitors of HIV-1 reverse transcriptase. Meleddu R, Cannas V, Distinto S, Sarais G, Del Vecchio C, Esposito F, Bianco G, Corona A, Cottiglia F, Alcaro S, Parolin C, Artese A, Scalise D, Fresta M, Arridu A, Ortuso F, Maccioni E, Tramontano E.ChemMedChem. 2014 Aug;9(8):1869-79. doi: 10.1002/cmdc.201402015.
32. Inhibition of foamy virus reverse transcriptase by human immunodeficiency virus type 1 RNase H inhibitors.Corona A, Schneider A, Schweimer K, Rösch P, Wöhrl BM, Tramontano E. Antimicrob Agents Chemother. 2014 Jul;58(7):4086-93. doi: 10.1128/AAC.00056-14.
33. Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.Costi R, Métifiot M, Chung S, Cuzzucoli Crucitti G, Maddali K, Pescatori L, Messore A, Madia VN, Pupo G, Scipione L, Tortorella S, Di Leva FS, Cosconati S, Marinelli L, Novellino E, Le Grice SF, Corona A, Pommier Y, Marchand C, Di Santo R. J Med Chem. 2014 Apr 24;57(8):3223-34. doi: 10.1021/jm5001503.
34. Active site and allosteric inhibitors of the ribonuclease H activity of HIV reverse transcriptase. Corona A, Masaoka T, Tocco G, Tramontano E, Le Grice SF. Future Med Chem. 2013 Dec;5(18):2127-39. doi: 10.4155/fmc.13.178.
35. Hypericum hircinum L. components as new single-molecule inhibitors of both HIV-1 reverse transcriptase-associated DNA polymerase and ribonuclease H activities. Esposito F, Sanna C, Del Vecchio C, Cannas V, Venditti A, Corona A, Bianco A, Serrilli AM, Guarcini L, Parolin C, Ballero M, Tramontano E. Pathog Dis. 2013 Aug;68(3):116-24. doi: 10.1111/2049-632X.12051.
36. New anthraquinone derivatives as inhibitors of the HIV-1 reverse transcriptase-associated ribonuclease H function.Esposito F, Corona A, Zinzula L, Kharlamova T, Tramontano E. Chemotherapy. 2012;58(4):299-307. doi: 10.1159/000343101. Epub 2012 Oct 31.
37. Molecular aspects of the RT/drug interactions. Perspective of dual inhibitors. Distinto S, Maccioni E, Meleddu R, Corona A, Alcaro S, Tramontano E.Curr Pharm Des. 2013;19(10):1850-9. Review.
38. HIV-1 Reverse Transcriptase Still Remains a New Drug Target: Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of Actions.Esposito F, Corona A, Tramontano E. Mol Biol Int. 2012;2012:586401. doi: 10.1155/2012/586401
39. Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity. Suchaud V, Bailly F, Lion C, Tramontano E, Esposito F, Corona A, Christ F, Debyser Z, Cotelle P. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3988-92. doi: 10.1016/j.bmcl.2012.04.096.
40. Alizarine derivatives as new dual inhibitors of the HIV-1 reverse transcriptase-associated DNA polymerase and RNase H activities effective also on the RNase H activity of non-nucleoside resistant reverse transcriptases. Esposito F, Kharlamova T, Distinto S, Zinzula L, Cheng YC, Dutschman G, Floris G, Markt P, Corona A, Tramontano E. FEBS J. 2011 May;278(9):1444-57. doi: 10.1111/j.1742-4658.2011.08057. PMID: 21348941