G proteins as drug targets

被引:61
作者
Höller, C [1 ]
Freissmuth, M [1 ]
Nanoff, C [1 ]
机构
[1] Univ Vienna, Inst Pharmacol, A-1090 Vienna, Austria
关键词
G protein subunits; modified guanine nucleotides; receptor-derived peptides; mastoparan and related venoms; suramin analogues; amphiphilic cations;
D O I
10.1007/s000180050288
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The structure and function of heterotrimeric G protein subunits is known in considerable detail. Upon stimulation of a heptahelical receptor by the appropriate agonists, the cognate G proteins undergo a cycle of activation and deactivation; the alpha-subunits and the beta gamma-dimers interact sequentially with several reaction partners (receptor, guanine nucleotides and effecters as well as regulatory proteins) by exposing appropriate binding sites. For most of these domains, low molecular weight ligands have been identified that either activate or inhibit signal transduction. These ligands include short peptides derived from receptors, G protein subunits and effecters, mastoparan and related insect venoms, modified guanine nucleotides, suramin analogues and amphiphilic cations. Because compounds that act on G proteins may be endowed with new forms of selectivity, we propose that G protein subunits may therefore be considered as potential drug targets.
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页码:257 / 270
页数:14
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