Results 41 to 50 of about 27,101 (273)

Hydroxymethylglutaryl CoA reductase and the modulation of microsomal cholesterol content by the nonspecific lipid transfer protein.

open access: yesJournal of Lipid Research, 1984
The influence of membrane cholesterol content on 3-hydroxy-3-methylglutaryl CoA reductase (HMG-CoA reductase, EC 1.1.1.34) in rat liver microsomes was investigated.
G P van Heusden, K W Wirtz
doaj   +1 more source

CYP1A2 is the major isoform responsible for paeonol O-demethylation in human liver microsomes

open access: yes, 2009
1. Paeonol, the primary active component of a traditional Chinese medicine Moutan Cortex, has a wide range of pharmacological activities. In the present study, the metabolism of paeonol by cytochrome P450s (CYPs) was investigated in human liver ...
Hu, Y.   +6 more
core   +1 more source

An integrated study for the utilization of anthraquinone compounds extract “Heshouwu” In vivo and their comparative metabolism in liver microsomes using UPLC-ESI-Q-TOF/MSn

open access: yesWorld Journal of Traditional Chinese Medicine, 2018
Objective: Anthraquinone (AQ), a major bioactive component of the traditional Chinese medicine HeShouWu, has widespread applications in industry and medicine.
Sha Chen   +6 more
doaj   +1 more source

A comprehensive characterization biotransformation of chlorinated paraffin by human and carp liver microsomes via liquid chromatography-high-resolution mass spectrometry and screening algorithm

open access: yesEnvironment International
The chlorinated paraffin (CP) monomer 1,2,5,6,9,10-Hexachlorodecane (CP-4) was subjected to in vitro biotransformation using human and carp liver microsomes.
Liujun Chen   +5 more
doaj   +1 more source

Inhibition of human liver microsomal CYP by nateglinide

open access: yesJournal of Pharmacy and Pharmacology, 2010
AbstractObjectivesNateglinide is metabolized by CYP2C9 and CYP3A4, therefore drug–drug interactions through cytochrome P450 (CYP) inhibition may occur. In this study, we examined the inhibitory effects of nateglinide and its major metabolite N-[trans-4-(1-hydroxy-1-methylethyl)-cyclohexanecarbonyl]-d-phenylalanine (M1) on various CYP isoforms in human ...
Toshiyuki, Takanohashi   +4 more
openaire   +2 more sources

Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors

open access: yesAdvanced Science, EarlyView.
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng   +12 more
wiley   +1 more source

A Microgel Platform Enables Site‐Specific Intestinal Delivery of Lactoferrin, Improving its Bioavailability for Targeted Alleviating Liver Injury and Colitis

open access: yesAdvanced Science, EarlyView.
This work first time reports an eco‐friendly desert plant food‐based polysaccharide ASKP microgels which have intestinal site‐specific release properties which can achieve small‐intestine or colon targeting capability via different cross‐linking chemistry.
Huiling Yan   +10 more
wiley   +1 more source

In Vitro Metabolism and In Vivo Pharmacokinetics Profiles of Hydroxy-α-Sanshool

open access: yesToxics
Hydroxy-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

Characterization of triptolide hydroxylation by cytochrome P450 in human and rat liver microsomes

open access: yes, 2008
Triptolide, the primary active component of a traditional Chinese medicine Tripterygium wilfordii Hook F, has a wide range of pharmacological activities. In the present study, the metabolism of triptolide by cytochrome P450s was investigated in human and
Liu, H. -T.   +13 more
core   +1 more source

AI‐Designed Cyclic Peptides Enable Controllable Modulation of the CD28 Immune Checkpoint

open access: yesAdvanced Science, EarlyView.
AI‐designed cyclic peptides enable controllable modulation of the CD28 immune checkpoint through reversible disruption of CD28‐CD80/CD86 interactions. The lead peptide, CIP‐3, suppresses T‐cell activation without intrinsic agonist activity, demonstrates dose‐dependent efficacy in a murine colitis model, and attenuates inflammatory cytokine production ...
Katarzyna Kuncewicz   +4 more
wiley   +1 more source

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