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                                                Global Journal of Biochemistry. Volume 2, Issue 1 (2011)  pp. 59-73
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                                                Research Article
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                                                Free Article
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                                                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
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                                                Alexander O. Shpakova, Elena A. Shpakovab, Irina I. Tarasenkob, Kira V. Derkacha,
Oksana V. Chistyakovaa, Elena V. Avdeevac, Gennady P. Vlasovb
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                                                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
                                                 
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                                                Abstract | 
                                            
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                                                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. 
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                                                Keywords | 
                    
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                        Adenylyl cyclase, GTP-binding protein, Peptide, Luteinizing hormone receptor, Third intracellular loop, Chorionic gonadotropin
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