Mechanisms of inverse agonism at G-protein-coupled receptors.
Mechanisms of inverse agonism at G-protein-coupled receptors.
复制标题
G 蛋白偶联受体的反向激动机制。
DOI：
10.1016/s0165-6147(02)01993-4
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发表时间：
2002
影响因子：
13.8
通讯作者：
P. Strange
中科院分区：
文献类型：
--
作者：
P. Strange
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Many drugs with important therapeutic actions that had been assumed to be antagonists at G-protein-coupled receptors (GPCRs) have been shown to be inverse agonists. For both basic pharmacology and drug design it is important to understand the mechanisms whereby these drugs achieve their effects. It had been assumed that these drugs achieved their effects by stabilizing an inactive state of the receptor (R) at the expense of a partially activated state (R*). In this article, I consider this and other mechanisms that could explain inverse agonist actions, and conclude that more than one mechanism can apply to inverse agonism at GPCRs.
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DOI：
10.1016/s0021-9258(18)53442-6
发表时间：
1993-03
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
P. Samama;S. Cotecchia;T. Costa;R. Lefkowitz
通讯作者：
P. Samama;S. Cotecchia;T. Costa;R. Lefkowitz
组成型活性 1 型甲状旁腺激素受体的选择性和非选择性反向激动剂：受体构象改变的证据。
DOI：
10.1210/endo.142.4.8103
发表时间：
2001
期刊：
Endocrinology.
影响因子：
--
作者：
Carter,PH;Petroni,BD;Gensure,RC;Schipani,E;PottsJr,JT;Gardella,TJ
通讯作者：
Gardella,TJ
影响因子：
3.6
作者：
DeLean,A;Kilpatrick,BF;Caron,MG
通讯作者：
Caron,MG
5-羟色胺 2C 型受体激动剂和反向激动剂的相互结合特性。
影响因子：
3.6
作者：
Westphal,RS;Sanders-Bush,E
通讯作者：
Sanders-Bush,E
负拮抗剂促进β2-肾上腺素能受体的失活构象。
影响因子：
3.6
作者：
Samama,P;Pei,G;Costa,T;Cotecchia,S;Lefkowitz,RJ
通讯作者：
Lefkowitz,RJ