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A small molecule compound with an indole moiety inhibits the main protease of SARS-CoV-2 and blocks virus replication.
Hattori SI, Higashi-Kuwata N, Hayashi H, Allu SR, Raghavaiah J, Bulut H, Das D, Anson BJ, Lendy EK, Takamatsu Y, Takamune N, Kishimoto N, Murayama K, Hasegawa K, Li M, Davis DA, Kodama EN, Yarchoan R, Wlodawer A, Misumi S, Mesecar AD, Ghosh AK, Mitsuya H. Hattori SI, et al. Among authors: bulut h. Nat Commun. 2021 Jan 28;12(1):668. doi: 10.1038/s41467-021-20900-6. Nat Commun. 2021. PMID: 33510133 Free PMC article.
A Modified P1 Moiety Enhances In Vitro Antiviral Activity against Various Multidrug-Resistant HIV-1 Variants and In Vitro Central Nervous System Penetration Properties of a Novel Nonpeptidic Protease Inhibitor, GRL-10413.
Amano M, Salcedo-Gómez PM, Zhao R, Yedidi RS, Das D, Bulut H, Delino NS, Sheri VR, Ghosh AK, Mitsuya H. Amano M, et al. Among authors: bulut h. Antimicrob Agents Chemother. 2016 Nov 21;60(12):7046-7059. doi: 10.1128/AAC.01428-16. Print 2016 Dec. Antimicrob Agents Chemother. 2016. PMID: 27620483 Free PMC article.
Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants.
Ghosh AK, Rao KV, Nyalapatla PR, Osswald HL, Martyr CD, Aoki M, Hayashi H, Agniswamy J, Wang YF, Bulut H, Das D, Weber IT, Mitsuya H. Ghosh AK, et al. Among authors: bulut h. J Med Chem. 2017 May 25;60(10):4267-4278. doi: 10.1021/acs.jmedchem.7b00172. Epub 2017 Apr 18. J Med Chem. 2017. PMID: 28418652 Free PMC article.
A novel central nervous system-penetrating protease inhibitor overcomes human immunodeficiency virus 1 resistance with unprecedented aM to pM potency.
Aoki M, Hayashi H, Rao KV, Das D, Higashi-Kuwata N, Bulut H, Aoki-Ogata H, Takamatsu Y, Yedidi RS, Davis DA, Hattori SI, Nishida N, Hasegawa K, Takamune N, Nyalapatla PR, Osswald HL, Jono H, Saito H, Yarchoan R, Misumi S, Ghosh AK, Mitsuya H. Aoki M, et al. Among authors: bulut h. Elife. 2017 Oct 17;6:e28020. doi: 10.7554/eLife.28020. Elife. 2017. PMID: 29039736 Free PMC article.
Halogen Bond Interactions of Novel HIV-1 Protease Inhibitors (PI) (GRL-001-15 and GRL-003-15) with the Flap of Protease Are Critical for Their Potent Activity against Wild-Type HIV-1 and Multi-PI-Resistant Variants.
Hattori SI, Hayashi H, Bulut H, Rao KV, Nyalapatla PR, Hasegawa K, Aoki M, Ghosh AK, Mitsuya H. Hattori SI, et al. Among authors: bulut h. Antimicrob Agents Chemother. 2019 May 24;63(6):e02635-18. doi: 10.1128/AAC.02635-18. Print 2019 Jun. Antimicrob Agents Chemother. 2019. PMID: 30962341 Free PMC article.
Novel Protease Inhibitors Containing C-5-Modified bis-Tetrahydrofuranylurethane and Aminobenzothiazole as P2 and P2' Ligands That Exert Potent Antiviral Activity against Highly Multidrug-Resistant HIV-1 with a High Genetic Barrier against the Emergence of Drug Resistance.
Takamatsu Y, Aoki M, Bulut H, Das D, Amano M, Sheri VR, Kovari LC, Hayashi H, Delino NS, Ghosh AK, Mitsuya H. Takamatsu Y, et al. Among authors: bulut h. Antimicrob Agents Chemother. 2019 Jul 25;63(8):e00372-19. doi: 10.1128/AAC.00372-19. Print 2019 Aug. Antimicrob Agents Chemother. 2019. PMID: 31085520 Free PMC article.
GRL-0920, an Indole Chloropyridinyl Ester, Completely Blocks SARS-CoV-2 Infection.
Hattori SI, Higshi-Kuwata N, Raghavaiah J, Das D, Bulut H, Davis DA, Takamatsu Y, Matsuda K, Takamune N, Kishimoto N, Okamura T, Misumi S, Yarchoan R, Maeda K, Ghosh AK, Mitsuya H. Hattori SI, et al. Among authors: bulut h. mBio. 2020 Aug 20;11(4):e01833-20. doi: 10.1128/mBio.01833-20. mBio. 2020. PMID: 32820005 Free PMC article.
Identification of a novel long-acting 4'-modified nucleoside reverse transcriptase inhibitor against HBV.
Higashi-Kuwata N, Hayashi S, Kumamoto H, Ogata-Aoki H, Das D, Venzon D, Hattori SI, Bulut H, Hashimoto M, Otagiri M, Takamune N, Kishimoto N, Davis DA, Misumi S, Kakuni M, Tanaka Y, Mitsuya H. Higashi-Kuwata N, et al. Among authors: bulut h. J Hepatol. 2021 May;74(5):1075-1086. doi: 10.1016/j.jhep.2020.12.006. Epub 2020 Dec 15. J Hepatol. 2021. PMID: 33333207 Free PMC article.
259 results