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

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Abstract

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. Recent 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 the functional activity of intracellular signaling cascades and fundamental cellular processes controlled by them. GPCR-derived 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 great prospects in the development of the new generations of drugs based on GPCR-derived peptides, which can regulate the important functions of the organism.

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Abbreviations

AR:

adrenergic receptor

ICL:

intracellular loop

GPCR:

G protein-coupled receptors

PAR:

protease activated receptors

PLCβ:

phospholipase Cβ

S1P3-R:

sphingosine-1-phosphate receptor 3

TM:

transmembrane region

TSH:

thyroid stimulating hormone

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Authors and Affiliations

  1. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, ul. Thoreza 44, St. Petersburg, 194223, Russia

    A. O. Shpakov

  2. Institute of Macromolecular Compounds, Russian Academy of Sciences, Bolshoi pr. 31, St. Petersburg, 199004, Russia

    E. A. Shpakova

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  1. A. O. Shpakov
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  2. E. A. Shpakova
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Correspondence to A. O. Shpakov.

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Original Russian Text © A.O. Shpakov, E.A. Shpakova, 2014, published in Biomeditsinskaya Khimiya.

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Shpakov, A.O., Shpakova, E.A. Prospects for the use of peptides and their derivatives, structurally corresponding to the g protein-coupled receptors, in medicine. Biochem. Moscow Suppl. Ser. B 8, 19–26 (2014). https://doi.org/10.1134/S1990750814010144

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