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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. 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.
However, highly DRV-resistant variants have been reported in patients receiving long-term DRV-containing regimens. Here, we report three novel HIV-1 PIs (GRL-057-14, GRL-058-14, and GRL-059-14), all of which contain a P2-amino-substituted-bis-tetrahydrofuranylurethane (bis …
However, highly DRV-resistant variants have been reported in patients receiving long-term DRV-containing regimens. Here, we report th …
Novel Central Nervous System (CNS)-Targeting Protease Inhibitors for Drug-Resistant HIV Infection and HIV-Associated CNS Complications.
Amano M, Salcedo-Gómez PM, Yedidi RS, Zhao R, Hayashi H, Hasegawa K, Nakamura T, Martyr CD, Ghosh AK, Mitsuya H. Amano M, et al. Antimicrob Agents Chemother. 2019 Jun 24;63(7):e00466-19. doi: 10.1128/AAC.00466-19. Print 2019 Jul. Antimicrob Agents Chemother. 2019. PMID: 31061155 Free PMC article.
Such CNS-targeting PIs maintained their antiviral activity against HIV-2(ROD) as well as multidrug-resistant clinical HIV-1 variants isolated from AIDS patients who no longer responded to existing antiviral regimens after long-term therapy. Long-term drug selection …
Such CNS-targeting PIs maintained their antiviral activity against HIV-2(ROD) as well as multidrug-resistant clinical HIV-1 variants isolate …
GRL-09510, a Unique P2-Crown-Tetrahydrofuranylurethane -Containing HIV-1 Protease Inhibitor, Maintains Its Favorable Antiviral Activity against Highly-Drug-Resistant HIV-1 Variants in vitro.
Amano M, Miguel Salcedo-Gómez P, Yedidi RS, Delino NS, Nakata H, Venkateswara Rao K, Ghosh AK, Mitsuya H. Amano M, et al. Sci Rep. 2017 Sep 25;7(1):12235. doi: 10.1038/s41598-017-12052-9. Sci Rep. 2017. PMID: 28947797 Free PMC article.
Under the selection condition, where HIV-1(NL4-3) rapidly acquired significant resistance to APV, an integrase inhibitor raltegravir, and a GRL-09510 congener (GRL-09610), no variants highly resistant against GRL-09510 emerged over long-term in vitro passage of the virus. …
Under the selection condition, where HIV-1(NL4-3) rapidly acquired significant resistance to APV, an integrase inhibitor raltegravir, and a …
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. 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.
GRL-10413 also maintained its strong antiviral activity against multidrug-resistant clinical HIV-1 variants isolated from patients who no longer responded to various antiviral regimens after long-term antiretroviral therapy. The development of resistance against GRL-10413 …
GRL-10413 also maintained its strong antiviral activity against multidrug-resistant clinical HIV-1 variants isolated from patients who no lo …
A novel tricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor, GRL-0739, effectively inhibits the replication of multidrug-resistant HIV-1 variants and has a desirable central nervous system penetration property in vitro.
Amano M, Tojo Y, Salcedo-Gómez PM, Parham GL, Nyalapatla PR, Das D, Ghosh AK, Mitsuya H. Amano M, et al. Antimicrob Agents Chemother. 2015 May;59(5):2625-35. doi: 10.1128/AAC.04757-14. Epub 2015 Feb 17. Antimicrob Agents Chemother. 2015. PMID: 25691652 Free PMC article.
GRL-0739 was also highly active against multidrug-resistant clinical HIV-1 variants isolated from patients who no longer responded to existing antiviral regimens after long-term antiretroviral therapy, as well as against the HIV-2ROD variant. ...
GRL-0739 was also highly active against multidrug-resistant clinical HIV-1 variants isolated from patients who no longer responded to existi …
GRL-0519, a novel oxatricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor (PI), potently suppresses replication of a wide spectrum of multi-PI-resistant HIV-1 variants in vitro.
Amano M, Tojo Y, Salcedo-Gómez PM, Campbell JR, Das D, Aoki M, Xu CX, Rao KV, Ghosh AK, Mitsuya H. Amano M, et al. Antimicrob Agents Chemother. 2013 May;57(5):2036-46. doi: 10.1128/AAC.02189-12. Epub 2013 Feb 12. Antimicrob Agents Chemother. 2013. PMID: 23403426 Free PMC article.
GRL-0519 was also potent against multi-PI-resistant clinical HIV-1 variants isolated from patients who no longer responded to existing antiviral regimens after long-term antiretroviral therapy, highly darunavir (DRV)-resistant variants, and HIV-2ROD. ...
GRL-0519 was also potent against multi-PI-resistant clinical HIV-1 variants isolated from patients who no longer responded to existing antiv …
Enhancing protein backbone binding--a fruitful concept for combating drug-resistant HIV.
Ghosh AK, Anderson DD, Weber IT, Mitsuya H. Ghosh AK, et al. Angew Chem Int Ed Engl. 2012 Feb 20;51(8):1778-802. doi: 10.1002/anie.201102762. Epub 2012 Jan 31. Angew Chem Int Ed Engl. 2012. PMID: 22290878 Free PMC article. Review.
This loss of potency has raised serious questions with regard to effective long-term antiretroviral therapy for HIV/AIDS. In this context, our research has focused on designing inhibitors that form extensive hydrogen-bonding interactions with the enzyme's backbone in the a …
This loss of potency has raised serious questions with regard to effective long-term antiretroviral therapy for HIV/AIDS. In this con …
Inhibition of anthrax lethal factor: lability of hydroxamate as a chelating group.
Li F, Chvyrkova I, Terzyan S, Wakeham N, Turner R, Ghosh AK, Zhang XC, Tang J. Li F, et al. Appl Microbiol Biotechnol. 2012 May;94(4):1041-9. doi: 10.1007/s00253-012-3893-7. Epub 2012 Jan 25. Appl Microbiol Biotechnol. 2012. PMID: 22270239 Free PMC article.
To resist this unique hydrolytic activity of LF, we further designed a new inhibitor R9LF-2 which contained the same structure as R9LF-1 except replacing the hydroxamic acid group with N,O-dimethyl hydroxamic acid (DMHA), -N(CH(3))-O-CH(3). R9LF-2 was not hydrolyzed by LF in long …
To resist this unique hydrolytic activity of LF, we further designed a new inhibitor R9LF-2 which contained the same structure as R9LF-1 exc …
Beta-secretase inhibitor GRL-8234 rescues age-related cognitive decline in APP transgenic mice.
Chang WP, Huang X, Downs D, Cirrito JR, Koelsch G, Holtzman DM, Ghosh AK, Tang J. Chang WP, et al. FASEB J. 2011 Feb;25(2):775-84. doi: 10.1096/fj.10-167213. Epub 2010 Nov 8. FASEB J. 2011. PMID: 21059748 Free PMC article.
We demonstrated that the injected GRL-8234 effectively enters the brain and rapidly decreases soluble Abeta in the brain of Tg2576 mice. The rescue of cognition, which was observed only after long-term inhibitor treatment ranging from 5 to 7.5 mo, was associated with a dec …
We demonstrated that the injected GRL-8234 effectively enters the brain and rapidly decreases soluble Abeta in the brain of Tg2576 mice. The …