Literature DB >> 19146417

The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.

Berthold Wroblowski1, Mark J Wigglesworth, Philip G Szekeres, Graham D Smith, Shahzad S Rahman, Neville H Nicholson, Alison I Muir, Adrian Hall, Jag P Heer, Stephen L Garland, William J Coates.   

Abstract

The novel 7-transmembrane receptor MrgX1 is located predominantly in the dorsal root ganglion and has consequently been implicated in the perception of pain. Here we describe the discovery and optimization of a small molecule agonist and initial docking studies of this ligand into the receptor in order to provide a suitable lead and tool compound for the elucidation of the physiological function of the receptor.

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Year:  2009        PMID: 19146417     DOI: 10.1021/jm800962k

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


  5 in total

1.  The effect of inflammation on the expression and distribution of the MAS-related gene receptors MrgE and MrgF in the murine ileum.

Authors:  Leela R Avula; Roeland Buckinx; Katrien Alpaerts; Anna Costagliola; Dirk Adriaensen; Luc Van Nassauw; Jean-Pierre Timmermans
Journal:  Histochem Cell Biol       Date:  2011-09-13       Impact factor: 4.304

2.  Expression and distribution patterns of Mas-related gene receptor subtypes A-H in the mouse intestine: inflammation-induced changes.

Authors:  Leela Rani Avula; Roeland Buckinx; Herman Favoreel; Eric Cox; Dirk Adriaensen; Luc Van Nassauw; Jean-Pierre Timmermans
Journal:  Histochem Cell Biol       Date:  2013-03-17       Impact factor: 4.304

3.  Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1.

Authors:  Wandong Wen; Yan Wang; Zhe Li; Pang-Yen Tseng; Owen B McManus; Meng Wu; Min Li; Craig W Lindsley; Xinzhong Dong; Corey R Hopkins
Journal:  ChemMedChem       Date:  2014-09-10       Impact factor: 3.466

4.  Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors.

Authors:  Niyada Hin; Jesse Alt; Sarah C Zimmermann; Greg Delahanty; Dana V Ferraris; Camilo Rojas; Fengxian Li; Qin Liu; Xinzhong Dong; Barbara S Slusher; Takashi Tsukamoto
Journal:  Bioorg Med Chem       Date:  2014-09-19       Impact factor: 3.641

5.  Thieno[2,3-d]pyrimidine-Based Positive Allosteric Modulators of Human Mas-Related G Protein-Coupled Receptor X1 (MRGPRX1).

Authors:  Ilyas Berhane; Niyada Hin; Ajit G Thomas; Qian Huang; Chi Zhang; Vijayabhaskar Veeravalli; Ying Wu; Justin Ng; Jesse Alt; Camilo Rojas; Hiroe Hihara; Mika Aoki; Kyoko Yoshizawa; Tomoki Nishioka; Shuichi Suzuki; Shao-Qiu He; Qi Peng; Yun Guan; Xinzhong Dong; Srinivasa N Raja; Barbara S Slusher; Rana Rais; Takashi Tsukamoto
Journal:  J Med Chem       Date:  2022-02-04       Impact factor: 8.039

  5 in total

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