Literature DB >> 7980588

Binding and cAMP studies of melanotropin peptides with the cloned human peripheral melanocortin receptor, hMC1R.

C Haskell-Luevano1, H Miwa, C Dickinson, V J Hruby, T Yamada, I Gantz.   

Abstract

Binding and stimulation of cAMP by the melanotropin peptides alpha-MSH (alpha-melanocyte-stimulating hormone) and its superpotent analogues [Nle4, DPhe7]alpha-MSH (MT-I) and Ac-[Nle4,[formula: see text]alpha-MSH4-10-NH2 (MT-II) were undertaken to examine their respective properties on the human peripheral melanocyte melanocortin receptor, hMC1R. alpha-MSH was found to possess a binding IC50 value of 6.5 +/- 0.9 x 10(-9) M and cAMP EC50 value of 2.0 +/- 0.6 x 10(-9) M. MT-I possesses a binding IC50 value of 1.2 +/- 0.3 x 10(-9) M and a cAMP EC50 of 0.5 +/- 0.03 x 10(-9) M. MT-II possesses a binding IC50 of 0.57 +/- 0.08 x 10(-9) M and cAMP EC50 value of 0.20 +/- 0.05 x 10(-9) M.

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Year:  1994        PMID： 7980588     DOI： 10.1006/bbrc.1994.2581

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN： 0006-291X            Impact factor:   3.575


  13 in total

1.  Effects of macrocycle size and rigidity on melanocortin receptor-1 and -5 selectivity in cyclic lactam alpha-melanocyte-stimulating hormone analogs.

Authors:  Alexander V Mayorov; So-Yeop Han; Minying Cai; Matthew R Hammer; Dev Trivedi; Victor J Hruby
Journal:  Chem Biol Drug Des       Date:  2006-05       Impact factor: 2.817

2.  Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.

Authors:  James P Cain; Alexander V Mayorov; Minying Cai; Hui Wang; Bahar Tan; Kevin Chandler; YeonSun Lee; Ravil R Petrov; Dev Trivedi; Victor J Hruby
Journal:  Bioorg Med Chem Lett       Date:  2006-08-22       Impact factor: 2.823

3.  Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.

Authors:  Alexander V Mayorov; Minying Cai; Kevin B Chandler; Ravil R Petrov; April R Van Scoy; Zerui Yu; Dustin K Tanaka; Dev Trivedi; Victor J Hruby
Journal:  J Med Chem       Date:  2006-03-23       Impact factor: 7.446

4.  The melanocortin circuit in obese and lean strains of chicks.

Authors:  Gideon Hen; Sara Yosefi; Victoria Simchaev; Dmitry Shinder; Victor J Hruby; Miriam Friedman-Einat
Journal:  J Endocrinol       Date:  2006-08       Impact factor: 4.286

5.  Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.

Authors:  Alexander V Mayorov; Minying Cai; Erin S Palmer; Dustin K Tanaka; James P Cain; Matthew M Dedek; Bahar Tan; Dev Trivedi; Victor J Hruby
Journal:  Bioorg Med Chem Lett       Date:  2011-03-13       Impact factor: 2.823

6.  Divergence of cAMP signalling pathways mediating augmented nucleotide excision repair and pigment induction in melanocytes.

Authors:  Erin M Wolf Horrell; Stuart G Jarrett; Katharine M Carter; John A D'Orazio
Journal:  Exp Dermatol       Date:  2017-04-21       Impact factor: 3.960

7.  Solid-phase peptide head-to-side chain cyclodimerization: discovery of C(2)-symmetric cyclic lactam hybrid α-melanocyte-stimulating hormone (MSH)/agouti-signaling protein (ASIP) analogues with potent activities at the human melanocortin receptors.

Authors:  Alexander V Mayorov; Minying Cai; Erin S Palmer; Zhihua Liu; James P Cain; Josef Vagner; Dev Trivedi; Victor J Hruby
Journal:  Peptides       Date:  2010-08-03       Impact factor: 3.750

8.  Multiple N-methylation of MT-II backbone amide bonds leads to melanocortin receptor subtype hMC1R selectivity: pharmacological and conformational studies.

Authors:  Lucas Doedens; Florian Opperer; Minying Cai; Johannes G Beck; Matt Dedek; Erin Palmer; Victor J Hruby; Horst Kessler
Journal:  J Am Chem Soc       Date:  2010-06-16       Impact factor: 15.419

Review 9.  Organic chemistry and biology: chemical biology through the eyes of collaboration.

Authors:  Victor J Hruby
Journal:  J Org Chem       Date:  2009-12-18       Impact factor: 4.354

10.  Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.

Authors:  Hongchang Qu; Minying Cai; Alexander V Mayorov; Paolo Grieco; Morgan Zingsheim; Dev Trivedi; Victor J Hruby
Journal:  J Med Chem       Date:  2009-06-25       Impact factor: 7.446
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