Výsledky vyhledávání

Akademický článek

Direct binding of ledipasvir to HCV NS5A: mechanism of resistance to an HCV antiviral agent.

Autor: Hyock Joo Kwon, Weimei Xing, Katie Chan, Anita Niedziela-Majka, Katherine M Brendza, Thorsten Kirschberg, Darryl Kato, John O Link, Guofeng Cheng, Xiaohong Liu, Roman Sakowicz

Publikováno v: PLoS ONE, Vol 10, Iss 4, p e0122844 (2015)

Ledipasvir, a direct acting antiviral agent (DAA) targeting the Hepatitis C Virus NS5A protein, exhibits picomolar activity in replicon cells. While its mechanism of action is unclear, mutations that confer resistance to ledipasvir in HCV replicon ce

Externí odkaz: https://doaj.org/article/2ec4378953f54de7b0076a7adeb703bd

Zobrazit plný text záznamu

The Discovery of Velpatasvir (GS-5816): The Potent Pan-Genotypic Once-Daily Oral HCV NS5A Inhibitor in the Single-Tablet Regimens Epclusa and Vosevi®

Autor: John O. Link

Publikováno v: Topics in Medicinal Chemistry ISBN: 9783030283995

The initial approval of the single-tablet regimen (STR) Harvoni®, containing the hepatitis C virus (HCV) nonstructural 5A protein (NS5A) inhibitor ledipasvir and the nonstructural 5B protein (NS5B) nucleotide inhibitor sofosbuvir (SOF), provided a m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a6a78afbfd0b247fb81c87d6dbc4b961
https://doi.org/10.1007/7355_2019_67

Zobrazit plný text záznamu

In Vitro Antiviral Activity and Resistance Profile Characterization of the Hepatitis C Virus NS5A Inhibitor Ledipasvir

Autor: Mei Yu, Betty Peng, Simin Xu, Nikos Pagratis, Ruoyu Gong, William E. Delaney, Guofeng Cheng, Hadas Dvory-Sobol, Brian P. Doehle, Yang Tian, Bin Han, John O. Link, Yu-Jen Lee, Amoreena C. Corsa, Yili Xu, Hongmei Mo, Michel Perron

Publikováno v: Antimicrobial Agents and Chemotherapy. 60:1847-1853

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) infection. Here, we report key preclinical antiviral properties of LDV, including in vitro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b48fd0106c336f484a251b3aa4b1a765
https://doi.org/10.1128/aac.02524-15

Zobrazit plný text záznamu

Discovery of Ledipasvir (GS-5885): A Potent, Once-Daily Oral NS5A Inhibitor for the Treatment of Hepatitis C Virus Infection

Publikováno v: Journal of Medicinal Chemistry. 57:2033-2046

A new class of highly potent NS5A inhibitors with an unsymmetric benzimidazole-difluorofluorene-imidazole core and distal [2.2.1]azabicyclic ring system was discovered. Optimization of antiviral potency and pharmacokinetics led to the identification

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e01a36ec6ef38fbdea906289d7749e6
https://doi.org/10.1021/jm401499g

Zobrazit plný text záznamu

539. GS-CA2: A Novel, Potent, and Selective First-In-class Inhibitor of HIV-1 Capsid Function Displays Nonclinical Pharmacokinetics Supporting Long-Acting Potential in Humans

Autor: Schroeder Scott D, Tse Winston C, Raju Subramanian, Anna Chiu, Tomas Cihlar, George Stepan, William Rowe, Shekeba Ahmadyar, Kelly Wang, Tiffany Chan, John O. Link, Jim Zheng, Judy Mwangi, Bing Lu, Stephen R. Yant

Publikováno v: Open Forum Infectious Diseases

Background GS-CA2, an analog of GS-CA1, is a novel and selective inhibitor of HIV-1 capsid function. Safety and pharmacokinetics (PK) of GS-CA2 is currently being evaluated in healthy human subjects. Herein, we present the anti-HIV activity and noncl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1539c387d6b59a6e2467e677ae0d5f9a
http://europepmc.org/articles/PMC6254825

Zobrazit plný text záznamu

Preclinical Pharmacokinetics and First-in-Human Pharmacokinetics, Safety, and Tolerability of Velpatasvir, a Pangenotypic Hepatitis C Virus NS5A Inhibitor, in Healthy Subjects

Autor: John Ling, Brian P. Kearney, Erik Mogalian, John McNally, Lingling Han, Cheng Yong Yang, Diana M. Brainard, John O. Link, Polina German, Anita Mathias

Publikováno v: Antimicrobial agents and chemotherapy. 61(5)

Preclinical characterization of velpatasvir (VEL; GS-5816), an inhibitor of the hepatitis C virus (HCV) NS5A protein, demonstrated that it has favorable in vitro and in vivo properties, including potent antiviral activity against hepatitis C virus ge

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fde9dd1a362aa3df54bc8508628062aa
https://pubmed.ncbi.nlm.nih.gov/28193657

Zobrazit plný text záznamu

Clinical Resistance to Velpatasvir (GS-5816), a Novel Pan-Genotypic Inhibitor of the Hepatitis C Virus NS5A Protein

Autor: Diana M. Brainard, Hadas Dvory-Sobol, John McNally, Michael D. Miller, John O. Link, Angela Worth, Eric Lawitz, Brian P. Doehle, Hongmei Mo

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 GT6 HCV replicons. In a phase 1b 3-day monotherapy study, patients treated with a 150-mg d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f446baeeeaf17912db9d6df4f7f3b88
https://europepmc.org/articles/PMC4997818/

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání