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  Global Journal of Biochemistry. Volume 2, Issue 1 (2011) pp. 59-73
  Research Article Free Article
The influence of peptides corresponding to the third intracellular loop of luteinizing hormone receptor on basal and hormone stimulated activity of the adenylyl cyclase signaling system
  Alexander O. Shpakova, Elena A. Shpakovab, Irina I. Tarasenkob, Kira V. Derkacha, Oksana V. Chistyakovaa, Elena V. Avdeevac, Gennady P. Vlasovb  
a Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences Thorez av. 44 194223 St. Petersburg, Russia
b Institute of Macromolecular Compounds, Russian Academy of Sciences, Bol’shoj av. 31, 199004 St Petersburg, Russia
c Institute of Cytology, Russian Academy of Sciences, Tikhoretskii av. 4 194064 St Petersburg, Russia

  In many G protein-coupled receptors an important role in binding and activation of G proteins belongs to the C-terminal region of the third intracellular loop (C-ICL-3). We showed that synthesized by us peptides L-Nle-ATNKDTKIAKK-Nle-A558-572-amide, NKDTKIAKK-Nle-A562-572-K(Palm)-A-amide and (NKDTKIAKK-Nle-A562-572)2-KGGC(Acm)-amide, derivatives of C-ICL-3 of the rat luteinizing hormone/chorionic gonadotropin receptor (LH/CG-R) stimulate the basal adenylyl cyclase (AC) activity, selectively activate Gs proteins and in a receptor-specific manner decrease the stimulating effects of human CG on AC system in the rat testes and ovaries. The LHR-peptides are biologically active only in the presence of cognate receptor, since in the brain and myocardium, where LH/CG-R content is very low, LHR-peptides influence AC system very little. Our results demonstrate that LHR-peptides are selective regulators of gonadotropin-sensitive AC system in the reproductive tissues and strongly suggest that the region homologous to them is responsible for specific LH/CG-R interaction with Gs proteins.
  Adenylyl cyclase, GTP-binding protein, Peptide, Luteinizing hormone receptor, Third intracellular loop, Chorionic gonadotropin  

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