Rupintrivir Explained

Rupintrivir (AG-7088, Rupinavir) is a peptidomimetic antiviral drug which acts as a 3C and 3CL protease inhibitor.^{[1] [2] [3]} It was developed for the treatment of rhinoviruses,^{[4] [5]} and has subsequently been investigated for the treatment of other viral diseases including those caused by picornaviruses,^{[6] [7]} norovirus,^[8] and coronaviruses, such as SARS and COVID-19.^{[9] [10]}

See also

• 3CLpro-1
• Carmofur
• Ebselen
• GC376
• Theaflavin digallate

Notes and References

1. Dragovich PS, Prins TJ, Zhou R, Webber SE, Marakovits JT, Fuhrman SA, Patick AK, Matthews DA, Lee CA, Ford CE, Burke BJ, Rejto PA, Hendrickson TF, Tuntland T, Brown EL, Meador JW, Ferre RA, Harr JE, Kosa MB, Worland ST . 6 . Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 4. Incorporation of P1 lactam moieties as L-glutamine replacements . Journal of Medicinal Chemistry . 42 . 7 . 1213–24 . April 1999 . 10197965 . 10.1021/jm9805384 .
2. Santos MM, Moreira R . Michael acceptors as cysteine protease inhibitors . Mini Reviews in Medicinal Chemistry . 7 . 10 . 1040–50 . October 2007 . 17979807 . 10.2174/138955707782110105 .
3. Yuan S, Fan K, Chen Z, Sun Y, Hou H, Zhu L . Structure of the HRV-C 3C-Rupintrivir Complex Provides New Insights for Inhibitor Design . Virologica Sinica . February 2020 . 35 . 4 . 445–454 . 32103448 . 10.1007/s12250-020-00196-4 . 7462945 .
4. Patick AK, Binford SL, Brothers MA, Jackson RL, Ford CE, Diem MD, Maldonado F, Dragovich PS, Zhou R, Prins TJ, Fuhrman SA, Meador JW, Zalman LS, Matthews DA, Worland ST . 6 . In vitro antiviral activity of AG7088, a potent inhibitor of human rhinovirus 3C protease . Antimicrobial Agents and Chemotherapy . 43 . 10 . 2444–50 . October 1999 . 10.1128/AAC.43.10.2444 . 10508022 . 89498 .
5. Book: Jensen LM, Walker EJ, Jans DA, Ghildyal R . Rhinoviruses . Proteases of human rhinovirus: role in infection . Methods in Molecular Biology . 2015 . 1221 . 129–41 . 25261311 . 10.1007/978-1-4939-1571-2_10 . 978-1-4939-1570-5 .
6. Barnard DL . Current status of anti-picornavirus therapies . Current Pharmaceutical Design . 2006 . 12 . 11 . 1379–90 . 16611122 . 10.2174/138161206776361129 .
7. De Palma AM, Vliegen I, De Clercq E, Neyts J . Selective inhibitors of picornavirus replication . Medicinal Research Reviews . 28 . 6 . 823–84 . November 2008 . 18381747 . 10.1002/med.20125 . 1575335 .
8. Rocha-Pereira J, Nascimento MS, Ma Q, Hilgenfeld R, Neyts J, Jochmans D . The enterovirus protease inhibitor rupintrivir exerts cross-genotypic anti-norovirus activity and clears cells from the norovirus replicon . Antimicrobial Agents and Chemotherapy . 58 . 8 . 4675–81 . August 2014 . 24890597 . 10.1128/AAC.02546-13 . 4136040 .
9. Anand K, Ziebuhr J, Wadhwani P, Mesters JR, Hilgenfeld R . Coronavirus main proteinase (3CLpro) structure: basis for design of anti-SARS drugs . Science . 300 . 5626 . 1763–7 . June 2003 . 12746549 . 10.1126/science.1085658 . 2003Sci...300.1763A . free .
10. Liu C, Zhou Q, Li Y, Garner LV, Watkins SP, Carter LJ, Smoot J, Gregg AC, Daniels AD, Jervey S, Albaiu D . 6 . Research and Development on Therapeutic Agents and Vaccines for COVID-19 and Related Human Coronavirus Diseases . ACS Central Science . 2020 . 6 . 3 . 315–331 . 10.1021/acscentsci.0c00272 . 32226821 . 7094090 . free .