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Literature DB >> 12646021

Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.

Timothy F Herpin¹, Guixue Yu, Kenneth E Carlson, George C Morton, Ximao Wu, Liya Kang, Huji Tuerdi, Ashish Khanna, John S Tokarski, R Michael Lawrence, John E Macor.

Abstract

The melanocortin-1 receptor (MC-1R) is a G-protein-coupled receptor involved in inflammation and skin pigmentation. Compound 2 is the first highly potent and selective MC-1R small-molecule agonist reported. Compound 2 showed efficacy in an acute model of inflammation, which has demonstrated the role of MC-1R in modulation of inflammation.

Entities: Chemical Disease Gene

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Year: 2003 PMID： 12646021 DOI： 10.1021/jm025600i

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

14 in total

1. Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists.

Authors: Irina D Pogozheva; Biao-Xin Chai; Andrei L Lomize; Tung M Fong; David H Weinberg; Ravi P Nargund; Michael W Mulholland; Ira Gantz; Henry I Mosberg
Journal: Biochemistry Date: 2005-08-30 Impact factor: 3.162

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

Review 3. 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

4. The melanoma-linked "redhead" MC1R influences dopaminergic neuron survival.

Authors: Xiqun Chen; Hongxiang Chen; Waijiao Cai; Michael Maguire; Bailiu Ya; Fuxing Zuo; Robert Logan; Hui Li; Katey Robinson; Charles R Vanderburg; Yang Yu; Yinsheng Wang; David E Fisher; Michael A Schwarzschild
Journal: Ann Neurol Date: 2017-01-23 Impact factor: 10.422

5. The melanocortin MC(1) receptor agonist BMS-470539 inhibits leucocyte trafficking in the inflamed vasculature.

Authors: G Leoni; M-B Voisin; K Carlson; Sj Getting; S Nourshargh; M Perretti
Journal: Br J Pharmacol Date: 2010-03-19 Impact factor: 8.739

6. Selected melanocortin 1 receptor single-nucleotide polymorphisms differentially alter multiple signaling pathways.

Authors: J R Doyle; J P Fortin; M Beinborn; A S Kopin
Journal: J Pharmacol Exp Ther Date: 2012-04-30 Impact factor: 4.030

7. Opioid and melanocortin receptors: do they have overlapping pharmacophores?

Authors: Yeon Sun Lee; Richard S Agnes; James P Cain; Vinod Kulkarni; Minying Cai; Christine Salibay; Kathy Ciano; Ravil Petrov; Alexander Mayorov; Josef Vagner; Dev Trivedi; Peg Davis; Shou-wu Ma; Josephine Lai; Frank Porreca; Ruben Vardanyan; Victor J Hruby
Journal: Biopolymers Date: 2008 Impact factor: 2.505