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具有不同受体/G蛋白化学计量比的天然和重组G蛋白偶联受体系统之间的差异。

Differences between natural and recombinant G protein-coupled receptor systems with varying receptor/G protein stoichiometry.

作者信息

Kenakin T

机构信息

Department of Receptor Biochemistry, Glaxo Wellcome Research and Development, Triangle Park, NC 27709, USA.

出版信息

Trends Pharmacol Sci. 1997 Dec;18(12):456-64. doi: 10.1016/s0165-6147(97)01136-x.

Abstract

The increasing accessibility of genetically engineered receptor systems for the study of drug-receptor interaction has led to a corresponding increase in the testing of new drug entities in recombinant receptor systems. In this article Terry Kenakin illustrates some possible conditions within these recombinant systems where the relative stoichiometry of the receptors to other cellular components may differ from that found in natural systems and where this difference may lead to anomalies in drug testing.

摘要

用于研究药物-受体相互作用的基因工程受体系统越来越容易获得,这使得在重组受体系统中对新药实体进行测试的相应增加。在本文中,特里·凯纳金阐述了这些重组系统中一些可能的情况,即受体与其他细胞成分的相对化学计量可能与天然系统中发现的不同,以及这种差异可能如何导致药物测试中的异常情况。

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