【摘 要】
:
Human carboxylesterase 1 (hCE-1) are a representative B-esterase, involved in the hydrolysis of many endogenous and exogenous compounds and are thus respons
【机 构】
:
Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Dalian 116023
【出 处】
:
2015年第一届药代动力学朝阳论坛
论文部分内容阅读
Human carboxylesterase 1 (hCE-1) are a representative B-esterase, involved in the hydrolysis of many endogenous and exogenous compounds and are thus responsible for the activation of many prodrugs.Dysfunction of hCE-1 in body has been proved to be related to many diseases, such as atherosclerosis, obesity, hepatic steatosis, hyperlipidemia, and hepatocellular carcinoma.In our previous work, we found N-(4-methyl butyrate)-4-hydroxy-l,8-naphthalimide (NMHN) could be rapidly deesterified by esterases to (3-carboxy propyl)-4-hydroxy-1, 8-naphthalimide (NCHN), which is a highly selective fluorescent probe for human UDP-glucuronosyltransferase 1A1.This elicits our interest in identifying which esterase is responsible for the hydrolysis of NMHN.In the present study, the hydrolysis pathway (s) of NMHN was investigated by using pooled human liver microsome (HLM) and various species of recombinant enzymes with hydrolytic activity.
其他文献
Diosbulbin B (DIOB) is the most abundant component of Dioscorea bulbifera L.(DB), a traditional Chinese medicine herb.DIOB and DB extracts have been reporte
The recognition of the gut microbiota-host metabolic axis and its implications in human metabolic disease has highlighted the contribution of the gut microb
LAT1 overexpressed on membrane of various tumor cells, are potential targets for tumor-targeting therapy.This study aimed to develop a LAT1-mediated drug de
CPRC1 is a novel investigated proton pump inhibitor, which shows dramaticsuccess in the management of acid-related disorders.Now this drug is being develope
Prediction of human PK at the preclinical stage can aid: ① human efficacious dose prediction, ②) human safety risk assessment based on detailed pharmacoki
Trastuzumab Emtansine(T-DM1, KadcylaTM, Genentech Inc.) is an antibody-drug conjugate(ADC) that received US FDA approval in 2013 for the treatment of human
Fasiglifam (TAK-875), a selective G-protein-coupled receptor 40 agonist, was developed for the treatment of type 2 diabetes mellitus.However, its clinical d
Many furan-containing compounds have been reported to be toxic and/or carcinogenic.Furanoids occur in a wide range of fruits, herbs, foods, and beverages.Th
Drug metabolizing enzymes (DMEs) play important roles in mammalians for the synthesis, metabolism and excretion of various kinds of chemicals, including num
Herbal medicinal products belong to a main part of complementary and alternative medicine and have worldwide using integrated with conventional medicines fo