Search Results - "Link, John O."
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Discovery of Ledipasvir (GS-5885): A Potent, Once-Daily Oral NS5A Inhibitor for the Treatment of Hepatitis C Virus Infection
Published in Journal of medicinal chemistry (13-03-2014)“…A new class of highly potent NS5A inhibitors with an unsymmetric benzimidazole-difluorofluorene-imidazole core and distal [2.2.1]azabicyclic ring system was…”
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Clinical Resistance to Velpatasvir (GS-5816), a Novel Pan-Genotypic Inhibitor of the Hepatitis C Virus NS5A Protein
Published in Antimicrobial agents and chemotherapy (01-09-2016)“…Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to…”
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Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi
Published in Bioorganic & medicinal chemistry letters (15-08-2019)“…[Display omitted] Treatment of hepatitis C virus (HCV) infection has been historically challenging due the high viral genetic complexity wherein there are…”
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Direct binding of ledipasvir to HCV NS5A: mechanism of resistance to an HCV antiviral agent
Published in PloS one (09-04-2015)“…Ledipasvir, a direct acting antiviral agent (DAA) targeting the Hepatitis C Virus NS5A protein, exhibits picomolar activity in replicon cells. While its…”
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Discovery of velpatasvir (GS-5816): A potent pan-genotypic HCV NS5A inhibitor in the single-tablet regimens Vosevi® and Epclusa
Published in Bioorganic & medicinal chemistry letters (15-08-2019)“…[Display omitted] Direct-acting antiviral inhibitors have revolutionized the treatment of hepatitis C virus (HCV) infected patients. Herein is described the…”
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A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model
Published in Nature medicine (01-09-2019)“…People living with HIV (PLWH) have expressed concern about the life-long burden and stigma associated with taking pills daily and can experience medication…”
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Lenacapavir Exhibits Atropisomerism-Mechanistic Pharmacokinetics and Disposition Studies of Lenacapavir Reveal Intestinal Excretion as a Major Clearance Pathway
Published in The Journal of pharmacology and experimental therapeutics (18-09-2024)“…Lenacapavir (LEN), a long-acting injectable, is the first approved human immunodeficiency virus type 1 capsid inhibitor and one of a few Food and Drug…”
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A phase 1, randomized, placebo-controlled, 3-day, dose-ranging study of GS-5885, an NS5A inhibitor, in patients with genotype 1 hepatitis C
Published in Journal of hepatology (01-07-2012)“…Background & Aims GS-5885 is an inhibitor of the hepatitis C virus (HCV) NS5A protein and exhibits potent suppression of genotype 1 HCV replicons. The safety,…”
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In Vitro Antiviral Activity and Resistance Profile Characterization of the Hepatitis C Virus NS5A Inhibitor Ledipasvir
Published in Antimicrobial agents and chemotherapy (01-03-2016)“…Ledipasvir (LDV; GS-5885), a component of Harvoni (a fixed-dose combination of LDV with sofosbuvir [SOF]), is approved to treat chronic hepatitis C virus (HCV)…”
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A general, catalytic, and enantioselective synthesis of .alpha.-amino acids
Published in Journal of the American Chemical Society (01-02-1992)Get full text
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Discovery of Hepatitis B Virus Surface Antigen Suppressor GS-8873
Published in ACS medicinal chemistry letters (11-04-2024)“…Chronic hepatitis B (CHB) virus infection afflicts hundreds of millions of people and causes nearly one million deaths annually. The high levels of circulating…”
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A catalytic enantioselective synthesis of denopamine, a useful drug for congestive heart failure
Published in Journal of organic chemistry (01-01-1991)Get full text
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Asymmetric Synthesis and Stereochemical Assignment of RS-97613, a Potent Immunosuppressive and Antiinflammatory Agent
Published in Journal of organic chemistry (22-03-1996)Get full text
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Trapping of an IMP Dehydrogenase−Substrate Covalent Intermediate by Mycophenolic Acid
Published in Journal of the American Chemical Society (28-02-1996)Get full text
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Clinical targeting of HIV capsid protein with a long-acting small molecule
Published in Nature (London) (27-08-2020)“…Oral antiretroviral agents provide life-saving treatments for millions of people living with HIV, and can prevent new infections via pre-exposure prophylaxis 1…”
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Metal mediated protease inhibition: design and synthesis of inhibitors of the human cytomegalovirus (hCMV) protease
Published in Bioorganic & medicinal chemistry letters (16-10-2000)“…A versatile synthetic route to a novel series of bis-imidazolemethanes designed to inhibit the hCMV protease has been developed and a series of potential metal…”
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Advances in cathepsin S inhibitor design
Published in Current opinion in drug discovery & development (01-07-2006)“…Cathepsin S is expressed in antigen-presenting cells and plays a role in invariant chain processing and major histocompatibility complex class II (MHCII)…”
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Direct Binding of Ledipasvir to HCV NS5A: Mechanism of Resistance to an HCV Antiviral Agent: e0122844
Published in PloS one (01-04-2015)“…Ledipasvir, a direct acting antiviral agent (DAA) targeting the Hepatitis C Virus NS5A protein, exhibits picomolar activity in replicon cells. While its…”
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