PMID: 11341936May 9, 2001Paper

Detection of regions in the MC1 receptor of importance for the selectivity of the MC1 receptor super-selective MS04/MS05 peptides

Biochimica Et Biophysica Acta
R MucenieceJarl E S Wikberg

Abstract

We have investigated the ability of our earlier identified MS04-MS05 MSH-peptide analogues to bind to chimeric MC1-MC3 receptors. While the MS04 and MS05 peptides bind with nanomolar and sub-nanomolar affinities to the wild type MC1 receptor, they bind only with micromolar affinities for the wild type MC3 receptor, thus being the hitherto most MC1 receptor selective ligands. Upon exchanging portions involving transmembrane regions TM1, TM2-3, and TM6-7 of the MC1 receptor with corresponding portions of the MC3 receptor both of these peptides showed major losses of affinities. By contrast exchanges involving TM4-5 did not appreciably affect the affinity of either MS04 or MS05. Our data suggest that the binding pocket for the MS04-MS05 MSH-peptides is located between TM1-3 and TM6-7 of the melanocortin receptors.

References

Oct 1, 1986·Acta Pharmacologica Et Toxicologica·A Bergström, J E Wikberg
Feb 15, 1995·European Journal of Pharmacology·H B SchiöthV Chhajlani
Sep 1, 1996·Pharmacology & Toxicology·H B SchiöthJ E Wikberg
Dec 24, 1996·Biochemical and Biophysical Research Communications·H B SchiöthJ E Wikberg
Nov 5, 1997·The Journal of Biological Chemistry·M SzardeningsJ E Wikberg
Aug 15, 1998·Molecular and Cellular Endocrinology·H B SchiöthJ E Wikberg
Sep 3, 1998·European Journal of Pharmacology·J OosteromR A Adan
Aug 12, 1999·European Journal of Pharmacology·J E Wikberg

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Citations

Dec 21, 2010·Journal of Peptide Science : an Official Publication of the European Peptide Society·Timothy WeedenJohn L Dzuris
Jul 18, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Maurício MoraisM Angeles Jiménez
Feb 22, 2017·Frontiers in Endocrinology·Davids FridmanisJanis Klovins
Dec 22, 2007·Journal of Receptor and Signal Transduction Research·Jean-Philippe BapstAlex N Eberle

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