期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 16, 页码 3621-3628出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.06.051
关键词
Binding kinetics; Residence time; G-protein coupled receptors; Dipeptidyl peptidas 4; Cellular environment
资金
- Instituut voor de aanmoediging van innovatie door Wetenschap & Technologie in Vlaanderen
- Fonds voor Wetenschappelijk Onderzoek Vlaanderen
While historically 'in vitro' binding data were obtained by analyzing equilibrium experiments, kinetic data are increasingly appreciated to provide information on the time a particular compound remains bound to its target. This information is of biological importance to understand the molecular mechanism of a drug not only to evaluate the time a particular receptor/enzyme is blocked in the case of antagonists/ inhibitors but also to investigate its contribution to the efficacy to mediate signaling in the case of agonists. There is accumulating evidence that many drugs binding to either membrane-bound receptors or enzymes are found to display long duration of action which can be ascribed to slow dissociation from their target proteins. In the present review three such examples are discussed which encompass ligands that bind to membrane-bound proteins and from which it appears that the tight binding kinetics is influenced by the cellular/membrane environment of the target protein. (C) 2017 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据