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Research Article Open access CC BY 3.0

Peptides Corresponding to Intracellular Regions of GPCR as a New Generation of Selective Drugs

Alexander O. Shpakov

International Journal of Biochemistry Research & Review · pp. 380–400 · Published 21 Aug 2013

10.9734/IJBCRR/2013/5593

Abstract

In the G protein-coupled receptors (GPCRs) relatively short regions of their intracellular loops and cytoplasmic C-terminal domain are responsible for specific interaction with G-proteins. GPCR-derived peptides corresponding to these regions are able to influence the activity of signal pathways involving the cognate receptors. Modified by hydrophobic radicals, these peptides turn into their cell-penetrating analogs, pepducins, possessing the activity both in vitro and in vivo. This review is devoted to the analysis of the available data and the prospects for GPCR-peptides and their lipophilic derivatives to be used in experimental and clinical medicine in the treatment of vascular diseases, cancers, inflammation, and endocrine dysfunctions.

Angiogenesis cancer G protein-coupled receptor heterotrimeric G protein inflammation intracellular loop palmitate pepducin peptide

Cited by 3

New achievements in development and application of GPCR-peptides

A. O. Shpakov, K. V. Derkach · Journal of Evolutionary Biochemistry and Physiology · 2015

Palmitoylated Peptide 562-572 of Luteinizing Hormone Receptor Increases Testosterone Level in Male Rats

K. V. Derkach, E. A. Shpakova, A. O. Shpakov · Bulletin of Experimental Biology and Medicine · 2014

Peptide 612–627 of thyrotropin receptor and its modified analogs as regulators of adenylyl cyclase in rat thyroid gland

A. O. Shpakov, E. A. Shpakova, I. I. Tarasenko · Cell and Tissue Biology · 2014

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