Shpakov Alexander O
I.M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, Thorez avenue 44, 194223 St. Petersburg, Russia.
J Amino Acids. 2011;2011:656051. doi: 10.4061/2011/656051. Epub 2011 Aug 23.
The functionally important regions of signal proteins participating in their specific interaction and responsible for transduction of hormonal signal into cell are rather short in length, having, as a rule, 8 to 20 amino acid residues. Synthetic peptides corresponding to these regions are able to mimic the activated form of full-size signal protein and to trigger signaling cascades in the absence of hormonal stimulus. They modulate protein-protein interaction and influence the activity of signal proteins followed by changes in their regulatory and catalytic sites. The present review is devoted to the achievements and perspectives of the study of signal protein-derived peptides and to their application as selective and effective regulators of hormonal signaling systems in vitro and in vivo. Attention is focused on the structure, biological activity, and molecular mechanisms of action of peptides, derivatives of the receptors, G protein α subunits, and the enzymes generating second messengers.
参与特定相互作用并负责将激素信号转导至细胞内的信号蛋白的功能重要区域长度相当短，通常含有8至20个氨基酸残基。与这些区域相对应的合成肽能够模拟全长信号蛋白的活化形式，并在没有激素刺激的情况下触发信号级联反应。它们调节蛋白质 - 蛋白质相互作用，并影响信号蛋白的活性，随后改变其调节和催化位点。本综述致力于信号蛋白衍生肽的研究成果与前景，以及它们在体外和体内作为激素信号系统的选择性有效调节剂的应用。重点关注肽、受体衍生物、G蛋白α亚基以及产生第二信使的酶的结构、生物活性和分子作用机制。
