The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
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.
Wroblowski
Berthold
B
GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park (North), Third Avenue, Harlow, Essex CM19 5AW, United Kingdom.
Wigglesworth
Mark J
MJ
Szekeres
Philip G
PG
Smith
Graham D
GD
Rahman
Shahzad S
SS
Nicholson
Neville H
NH
Muir
Alison I
AI
Hall
Adrian
A
Heer
Jag P
JP
Garland
Stephen L
SL
Coates
William J
WJ
D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D006801:Humans; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000502:physiology; D013329:Structure-Activity Relationship
D001713:Biphenyl Compounds; D010879:Piperazines; D011724:Pyridazines; D043562:Receptors, G-Protein-Coupled; C510803:mas-related gene-X1 receptor, human; D002118:Calcium