Results 91 to 100 of about 1,677,689 (317)
British Journal of Clinical Pharmacology, 1998 AIMS Chemical inhibitors of cytochrome P450 (CYP) are a useful tool in defining the role of individual CYPs involved in drug metabolism. The aim of the present study was to evaluate the selectivity and rank the order of potency of a range of isoform ...
V. Eagling, J. Tjia, D. Back
semanticscholar +1 more source
Molecular biomarkers and toxic consequences of impact by organic pollution in aquatic organisms [PDF]
, 1994 Organic contaminants are readily bioaccumulated by aquatic organisms. Exposure to and toxic effects of contaminants can be measured in terms of the biochemical responses of the organisms (i.e. molecular biomarkers).
Förlin, L. +2 more
core
Microsomal superoxide anion production and NADPH-oxidation in a series of 22 aziridinylbenzoquinones [PDF]
, 1989 Several 2,5-bis(1-aziridinyl)-1,4-benzoquinones (BABQs) can be activated to alkylating species by reduction of the quinone moiety. On the other hand, cytotoxicity of these compounds can be induced by redox cycling.
Koster, Andries Sj. +3 more
core +3 more sources
Chemistry – A European Journal, EarlyView.We present new BRD9‐targeting degraders featuring a chemical warhead and E3 ligase ligand that distinctly differ from the typical chemical units used for BRD9 degradation. Specifically, we identified two VHL‐based PROTACs (2 and 9) based on a [1,2,4]triazolo[4,3‐a]quinoxaline scaffold that effectively and selectively degrade BRD9 and exhibit ...
Martina Pierri +15 more
wiley +1 more source
The di-flavoenzyme reductase directly activates oxygen for the metabolism of diverse drug molecules by liver microsomal Cytochrome P450s [PDF]
arXiv, 2006 This submission has been withdrawn by arXiv administration due to complaints of misuse of institutional affiliation.
arxiv
ChemMedChem, EarlyView.Work presented here details the design and characterize novel G protein‐gated inwardly rectifying potassium channels (GIRK)1/2 activators. A new 4,4‐difluorocyclohexylpyrazole have been identified that confers improved potency and selectivity for GIRK1/2 versus GIRK1/4.
Sumaiya Nahid +8 more
wiley +1 more source
Journal of Traditional Chinese Medical Sciences, 2019 Objective: To explore the glucuronic acid metabolism of acacetin in human liver and intestinal microsomes to better characterize human uridine 5′-diphospho (UDP)-glucuronosyltransferase (UGT) isoforms. In addition, interspecies comparisons were performed
Kangle Shi, Shan Li, Qinggang Meng
doaj
In Vitro Metabolism and In Vivo Pharmacokinetics Profiles of Hydroxy-α-Sanshool
ToxicsHydroxy-α-sanshool (HAS) is the predominant active compound in Zanthoxylum bungeanum Maxim (ZBM). Our present work was aimed to explore the in vitro metabolism characteristics, and in vivo pharmacokinetic (PK) profile of HAS.
Jie Meng +4 more
doaj +1 more source
In Vitro Phase I Metabolism of CRV431, a Novel Oral Drug Candidate for Chronic Hepatitis B
Pharmaceutics, 2017 The cytochrome P450-mediated Phase I in vitro metabolism of CRV431 was studied using selective chemical inhibition and recombinant human enzymes. Additionally, the metabolic profile of CRV431 in human, rat, and monkey liver microsomes was investigated ...
Daniel J. Trepanier +2 more
doaj +1 more source
Pharmacology Research & Perspectives, 2022 UDP‐glucuronosyltransferases (UGTs) catalyze the conjugation of various substrates with sugars. Since the UGT2 family forms a large cluster spanning 1.5 Mb, transgenic mouse lines carrying the entire human UGT2 family have not been constructed because of
Kaoru Kobayashi +9 more
doaj +1 more source