Literature DB >> 21486697

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

Alexander V Mayorov1, Minying Cai, Erin S Palmer, Dustin K Tanaka, James P Cain, Matthew M Dedek, Bahar Tan, Dev Trivedi, Victor J Hruby.   

Abstract

A novel hybrid melanocortin pharmacophore was designed based on the topographical similarities between the pharmacophores of Agouti related protein (AGRP) an endogenous melanocortin antagonist, and α-melanocyte-stimulating hormone (α-MSH), an endogenous melanocortin agonist. When employed in two different 23-membered macrocyclic lactam peptide templates, the designed hybrid AGRP/MSH pharmacophore yielded non-competitive ligands with nanomolar range binding affinities. The topography-based pharmacophore hybridization strategy will prove useful in development of unique non-competitive melanocortin receptor modulators. Published by Elsevier Ltd.

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Year:  2011        PMID： 21486697      PMCID： PMC3216836          DOI： 10.1016/j.bmcl.2011.03.019

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  44 in total

Review 1.  Recent developments in our understanding of melanocortin system in the regulation of food intake.

Authors:  Y K Yang; C M Harmon
Journal:  Obes Rev       Date:  2003-11       Impact factor: 9.213

Review 2.  Melanocortin ligands: 30 years of structure-activity relationship (SAR) studies.

Authors:  Jerry Ryan Holder; Carrie Haskell-Luevano
Journal:  Med Res Rev       Date:  2004-05       Impact factor: 12.944

3.  Melanocortin receptor binding determinants in the agouti protein.

Authors:  L L Kiefer; J M Veal; K G Mountjoy; W O Wilkison
Journal:  Biochemistry       Date:  1998-01-27       Impact factor: 3.162

4.  Exocrine gland dysfunction in MC5-R-deficient mice: evidence for coordinated regulation of exocrine gland function by melanocortin peptides.

Authors:  W Chen; M A Kelly; X Opitz-Araya; R E Thomas; M J Low; R D Cone
Journal:  Cell       Date:  1997-12-12       Impact factor: 41.582

5.  Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.

Authors:  Andrzej Wilczynski; Xiang S Wang; Christine G Joseph; Zhimin Xiang; Rayna M Bauzo; Joseph W Scott; Nicholas B Sorensen; Amanda M Shaw; William J Millard; Nigel G Richards; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2004-04-22       Impact factor: 7.446

6.  Biological and conformational study of beta-substituted prolines in MT-II template: steric effects leading to human MC5 receptor selectivity.

Authors:  M Cai; C Cai; A V Mayorov; C Xiong; C M Cabello; V A Soloshonok; J R Swift; D Trivedi; V J Hruby
Journal:  J Pept Res       Date:  2004-02

7.  Solution structures of cyclic melanocortin agonists and antagonists by NMR.

Authors:  Jinfa Ying; Katalin E Kövér; Xuyuan Gu; Guoxia Han; Dev B Trivedi; Malcolm J Kavarana; Victor J Hruby
Journal:  Biopolymers       Date:  2003       Impact factor: 2.505

8.  alpha-Melanocyte-stimulating hormone inhibits lipopolysaccharide-induced tumor necrosis factor-alpha production in leukocytes by modulating protein kinase A, p38 kinase, and nuclear factor kappa B signaling pathways.

Authors:  Sun-Woo Yoon; Sung-Ho Goh; Jang-Soo Chun; Eun-Wie Cho; Myung-Kyu Lee; Kil-Lyong Kim; Jae-Jin Kim; Chul-Joong Kim; Haryoung Poo
Journal:  J Biol Chem       Date:  2003-06-19       Impact factor: 5.157

9.  Chimeric NDP-MSH and MTII melanocortin peptides with agouti-related protein (AGRP) Arg-Phe-Phe amino acids possess agonist melanocortin receptor activity.

Authors:  Christine G Joseph; Andrzej Wilczynski; Jerry R Holder; Zhimin Xiang; Rayna M Bauzo; Joseph W Scott; Carrie Haskell-Luevano
Journal:  Peptides       Date:  2003-12       Impact factor: 3.750

10.  4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity.

Authors:  T K Sawyer; P J Sanfilippo; V J Hruby; M H Engel; C B Heward; J B Burnett; M E Hadley
Journal:  Proc Natl Acad Sci U S A       Date:  1980-10       Impact factor: 11.205
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  2 in total

Review 1.  The Melanocortin Receptor System: A Target for Multiple Degenerative Diseases.

Authors:  Minying Cai; Victor J Hruby
Journal:  Curr Protein Pept Sci       Date:  2016       Impact factor: 3.272

2.  Demonstration of a Common DPhe7 to DNal(2')7 Peptide Ligand Antagonist Switch for Melanocortin-3 and Melanocortin-4 Receptors Identifies the Systematic Mischaracterization of the Pharmacological Properties of Melanocortin Peptides.

Authors:  Luis E Gimenez; Terry A Noblin; Savannah Y Williams; Satarupa Mullick Bagchi; Ren-Lei Ji; Ya-Xiong Tao; Claus B Jeppesen; Kilian W Conde-Frieboes; Tomi K Sawyer; Paolo Grieco; Roger D Cone
Journal:  J Med Chem       Date:  2022-04-11       Impact factor: 7.446
  2 in total

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