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  Global Journal of Biochemistry. Volume 2, Issue 2 (2011) pp. 96-123
  Review Article Free Article
GPCR-Based peptides: Structure, mechanisms of action and application
  Alexander O. Shpakov  
Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences St. Petersburg, Russia
  G protein-coupled receptors (GPCRs) activate large signaling networks that are integrating the information fluxes into appropriate biological responses and thus control the basic biochemical and physiological processes. One of the promising approaches used to study the structural-functional organization of GPCRs and the molecular mechanisms of their interaction with other signal proteins has been intensively developed in recent years in the frame of the peptide strategy based on the use of the synthetic peptides corresponding to the extracellular, intracellular and transmembrane regions of the receptors. Selectively regulating the functional activity of GPCR-dependent signaling cascades in vitro and in vivo these peptides may serve as therapeutic agents in the treatment of a wide range of diseases. In this review the data concerning the structure of GPCR-based peptides and the molecular mechanisms of their action are analyzed and their possible use in the development of new drugs is discussed.
  Extracellular loop; GTP-binding protein; G protein-coupled receptor; Intracellular loop; Peptide; Transmembrane region  

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