Literature DB >> 15027849

Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.

Tricia J Vos1, Andrei Caracoti, Jennifer L Che, Mingshi Dai, Cheryl A Farrer, Nancy E Forsyth, Stacey V Drabic, Robert A Horlick, Diana Lamppu, David L Yowe, Suresh Balani, Ping Li, Hang Zeng, Ingrid B J K Joseph, Luis E Rodriguez, Martin P Maguire, Michael A Patane, Christopher F Claiborne.   

Abstract

The melanocortin 4 receptor (MC4R) plays an important role in body weight regulation and energy homeostasis. Administration of peptidic MC4R antagonists (usually by intracerebro ventricular injection) has been shown in the literature to increase body weight and/or food intake in several rodent models. We report here the identification of a novel nonpeptidic MC4R antagonist and its effects on tumor-induced weight loss in mice following peripheral administration.

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Year:  2004        PMID： 15027849     DOI： 10.1021/jm034244g

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


  22 in total

Review 1.  Pharmacoperones: a new therapeutic approach for diseases caused by misfolded G protein-coupled receptors.

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2.  Failure-to-thrive syndrome associated with tumor formation by Madin-Darby canine kidney cells in newborn nude mice.

Authors:  Lauren R Brinster; Romelda L Omeir; Gideon S Foseh; Juliete N Macauley; Philip J Snoy; Joel J Beren; Belete Teferedegne; Keith Peden; Andrew M Lewis
Journal:  Comp Med       Date:  2013-08       Impact factor: 0.982

Review 3.  Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics.

Authors:  Ya-Xiong Tao
Journal:  Pharmacol Ther       Date:  2008-08-09       Impact factor: 12.310

Review 4.  The use of ghrelin and ghrelin receptor agonists as a treatment for animal models of disease: efficacy and mechanism.

Authors:  Mark D DeBoer
Journal:  Curr Pharm Des       Date:  2012       Impact factor: 3.116

5.  Liver cancer targeting of Doxorubicin with reduced distribution to the heart using hematoporphyrin-modified albumin nanoparticles in rats.

Authors:  Ji-Eun Chang; Won-Sik Shim; Su-Geun Yang; Eun-Young Kwak; Saeho Chong; Dae-Duk Kim; Suk-Jae Chung; Chang-Koo Shim
Journal:  Pharm Res       Date:  2011-10-05       Impact factor: 4.200

6.  The melanocortin-4 receptor: physiology, pharmacology, and pathophysiology.

Authors:  Ya-Xiong Tao
Journal:  Endocr Rev       Date:  2010-02-26       Impact factor: 19.871

7.  Melanocortin Receptor-4 and Glioblastoma Cells: Effects of the Selective Antagonist ML00253764 Alone and in Combination with Temozolomide In Vitro and In Vivo.

Authors:  Francesca Vaglini; Carla Pardini; Teresa Di Desidero; Paola Orlandi; Francesco Pasqualetti; Alessandra Ottani; Simone Pacini; Daniela Giuliani; Salvatore Guarini; Guido Bocci
Journal:  Mol Neurobiol       Date:  2017-08-08       Impact factor: 5.590

Review 8.  Update on melanocortin interventions for cachexia: progress toward clinical application.

Authors:  Mark Daniel DeBoer
Journal:  Nutrition       Date:  2009-12-08       Impact factor: 4.008

9.  Folding and Misfolding of Human Membrane Proteins in Health and Disease: From Single Molecules to Cellular Proteostasis.

Authors:  Justin T Marinko; Hui Huang; Wesley D Penn; John A Capra; Jonathan P Schlebach; Charles R Sanders
Journal:  Chem Rev       Date:  2019-01-04       Impact factor: 60.622

Review 10.  Design, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptor.

Authors:  Victor J Hruby; Minying Cai; James P Cain; Alexander V Mayorov; Matthew M Dedek; Devendra Trivedi
Journal:  Curr Top Med Chem       Date:  2007       Impact factor: 3.295
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