[HTML][HTML] Oral GS-441524 derivatives: Next-generation inhibitors of SARS‐CoV‐2 RNA‐dependent RNA polymerase

Z Wang, L Yang, X Song - Frontiers in Immunology, 2022 - frontiersin.org
GS-441524, an RNA‐dependent RNA polymerase (RdRp) inhibitor, is a 1′-CN-substituted
adenine C-nucleoside analog with broad-spectrum antiviral activity. However, the low oral …

[HTML][HTML] Potential herb‒drug interactions between anti-COVID-19 drugs and traditional Chinese medicine

L Ye, S Fan, P Zhao, C Wu, M Liu, S Hu, P Wang… - … Pharmaceutica Sinica B, 2023 - Elsevier
Abstract Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory
syndrome coronavirus 2 (SARS-CoV-2), has spread worldwide. Effective treatments against …

Viral target and metabolism‐based rationale for combined use of recently authorized small molecule COVID‐19 medicines: Molnupiravir, nirmatrelvir, and remdesivir

D Yan, B Yan - Fundamental & Clinical Pharmacology, 2023 - Wiley Online Library
The COVID‐19 pandemic remains a major health concern worldwide, and SARS‐CoV‐2 is
continuously evolving. There is an urgent need to identify new antiviral drugs and develop …

Discovery of seven-membered ring berberine analogues as highly potent and specific hCES2A inhibitors

Y Yang, Y Xiong, G Zhu, M Sun, K Zou, Y Zhao… - Chemico-Biological …, 2023 - Elsevier
Abstract Human carboxylesterase 2A (hCES2A) is a key serine hydrolase responsible for
the metabolic clearance of large number of compounds bearing the ester-or amide-bond (s) …

In vitro evaluation of the impact of Covid-19 therapeutic agents on the hydrolysis of the antiviral prodrug remdesivir

Q Zhang, PW Melchert, JS Markowitz - Chemico-Biological Interactions, 2022 - Elsevier
Abstract Remdesivir (RDV, Veklury®) is an FDA-approved prodrug for the treatment of
hospitalized patients with COVID-19. Recent in vitro studies have indicated that human …

Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to …

J Li, DM de Melo Jorge, W Wang, S Sun… - Journal of Medicinal …, 2024 - ACS Publications
We assessed factors that determine the tissue-specific bioactivation of ProTide prodrugs by
comparing the disposition and activation of remdesivir (RDV), its methylpropyl and isopropyl …

[HTML][HTML] The roles of serine hydrolases and serum albumin in alisol B 23-acetate hydrolysis in humans

T Zhang, F Zhang, Y Zhang, H Li, G Zhu… - Frontiers in …, 2023 - frontiersin.org
Introduction: Alisol B 23-acetate (AB23A), a major bioactive constituent in the Chinese herb
Zexie (Rhizoma Alismatis), has been found with multiple pharmacological activities. AB23A …

Human UDP-glucuronosyltransferase 1As catalyze aristolochic acid D O-glucuronidation to form a lesser nephrotoxic glucuronide

DZ Tu, PQ Liu, GH Zhu, HR Zeng, YY Deng… - Journal of …, 2024 - Elsevier
Abstract Ethnopharmacological relevance Aristolochic acids (AAs) are naturally occurring
nitro phenanthrene carboxylic acids primarily found in plants of the Aristolochiaceae family …

Regulation of human hydrolases and its implications in pharmacokinetics and pharmacodynamics

SM Jung, HJ Zhu - Drug Metabolism and Disposition, 2024 - ASPET
Hydrolases represent an essential class of enzymes indispensable for the metabolism of
various clinically essential medications. Individuals exhibit marked differences in the …

Regulation of carboxylesterases and its impact on pharmacokinetics and pharmacodynamics: an up-to-date review

Y Liu, J Li, HJ Zhu - Expert Opinion on Drug Metabolism & …, 2024 - Taylor & Francis
ABSTRACT Introduction Carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2) are
among the most abundant hydrolases in humans, catalyzing the metabolism of numerous …