Prospects for use of peptides and their derivatives, structurally corresponding to the G protein-coupled receptors, in medicine

   
Shpakov A.O.1 , Shpakova E.A.2

1. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, Saint Petersburg, Russia
2. Institute of Macromolecular Compounds, Russian Academy of Sciences, Saint Petersburg, Russia
Section: Review
DOI: 10.18097/PBMC20156101019      PubMed Id: 25762596
Year: 2015  Volume: 61  Issue: 1  Pages: 19-29
The regulation of signaling pathways involved in the control of many physiological functions is carried out via the heterotrimeric G protein-coupled receptors (GPCR). The search of effective and selective regulators of GPCR and intracellular signaling cascades coupled with them is one of the important problems of modern fundamental and clinical medicine. Recently data suggest that synthetic peptides and their derivatives, structurally corresponding to the intracellular and transmembrane regions of GPCR, can interact with high efficiency and selectivity with homologous receptors and influence, thus, the functional activity of intracellular signaling cascades and fundamental cellular processes controlled by them. GPCR-peptides are active in both in vitro and in vivo. They regulate hematopoiesis, angiogenesis and cell proliferation, inhibit tumor growth and metastasis, and prevent the inflammatory diseases and septic shock. These data show greatest prospects in the development of the new generations of drugs based on GPCR-derived peptides, capable of regulating the important functions of the organism.
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Keywords: angiogenesis, metastasis, tumor, pepducin, peptide, sepsis, G protein-coupled receptor, transmembrane region, thrombosis, intracellular loop
Citation:

Shpakov, A. O., Shpakova, E. A. (2015). Prospects for use of peptides and their derivatives, structurally corresponding to the G protein-coupled receptors, in medicine. Biomeditsinskaya khimiya, 61(1), 19-29.
This paper is also available as the English translation: 10.1134/S1990750814010144
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