Regulation of the Melanocortin-Sensitive Adenylate Cyclase System by N-Acylated Peptide 71-82 of Type 4 Melanocortin Receptor
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| 024 | 7 | 0 | |a 10.1007/s10517-015-3093-4 |2 doi |
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| 245 | 0 | 0 | |a Regulation of the Melanocortin-Sensitive Adenylate Cyclase System by N-Acylated Peptide 71-82 of Type 4 Melanocortin Receptor |h [Elektronische Daten] |c [A. Shpakov, K. Derkach, E. Shpakova] |
| 520 | 3 | |a The peptides structurally corresponding in to cytoplasmic loops of G protein-coupled receptors (GPCR) are able to control functional activity of homologous receptors and the corresponding signaling pathways. Modification of these peptides with hydrophobic radicals enhances their biological activity due to penetration of lipophilic derivatives through the membrane and anchoring near their targets, GPCR. We synthesized an N-palmitoylated peptide Palm-Val-[Lys-Asn-Lys-Asn-Leu-His-Ser-Pro-(Nle)-Tyr-Phe-Phe71-82]-amide-Palm-Val-(71-82) structurally corresponding to cytoplasmic loop 1 of melanocortin 4 receptor (M4R). We found that in micromolar concentrations it very effectively suppresses stimulation of basal adenylate cyclase activity and basal level of GppNHp binding of heterotrimeric G proteins produced by THIQ and α-melanocyte stimulating hormone (α-MSH), agonists of M4R homologous to the peptide, in synaptosomal membranes of rat brain. The peptide Palm-Val-(71-82) also reduced, albeit to a significantly less extent, stimulation of adenylate cyclase and G-proteins by M3R agonist of γ-MSH, due to high homology of the peptide primary structure to M3R cytoplasmic loop 1. The synthesized peptide with activity of M4R/M3R antagonist can be used for the development of regulators of M4R and M3R and the corresponding biochemical and physiological processes. | |
| 540 | |a Springer Science+Business Media New York, 2015 | ||
| 690 | 7 | |a adenylate cyclase |2 nationallicence | |
| 690 | 7 | |a melanocortin receptor |2 nationallicence | |
| 690 | 7 | |a brain |2 nationallicence | |
| 690 | 7 | |a peptide |2 nationallicence | |
| 690 | 7 | |a cytoplasmic loop 1 |2 nationallicence | |
| 700 | 1 | |a Shpakov |D A. |u Laboratory of Molecular Endocrinology, I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia |4 aut | |
| 700 | 1 | |a Derkach |D K. |u Laboratory of Molecular Endocrinology, I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia |4 aut | |
| 700 | 1 | |a Shpakova |D E. |u Laboratory of Molecular Endocrinology, I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia |4 aut | |
| 773 | 0 | |t Bulletin of Experimental Biology and Medicine |d Springer US; http://www.springer-ny.com |g 160/1(2015-11-01), 40-44 |x 0007-4888 |q 160:1<40 |1 2015 |2 160 |o 10517 | |
| 856 | 4 | 0 | |u https://doi.org/10.1007/s10517-015-3093-4 |q text/html |z Onlinezugriff via DOI |
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| 900 | 7 | |a Metadata rights reserved |b Springer special CC-BY-NC licence |2 nationallicence | |
| 908 | |D 1 |a research-article |2 jats | ||
| 949 | |B NATIONALLICENCE |F NATIONALLICENCE |b NL-springer | ||
| 950 | |B NATIONALLICENCE |P 856 |E 40 |u https://doi.org/10.1007/s10517-015-3093-4 |q text/html |z Onlinezugriff via DOI | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Shpakov |D A. |u Laboratory of Molecular Endocrinology, I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Derkach |D K. |u Laboratory of Molecular Endocrinology, I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia |4 aut | ||
| 950 | |B NATIONALLICENCE |P 700 |E 1- |a Shpakova |D E. |u Laboratory of Molecular Endocrinology, I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia |4 aut | ||
| 950 | |B NATIONALLICENCE |P 773 |E 0- |t Bulletin of Experimental Biology and Medicine |d Springer US; http://www.springer-ny.com |g 160/1(2015-11-01), 40-44 |x 0007-4888 |q 160:1<40 |1 2015 |2 160 |o 10517 | ||