Article
MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology - 1 May 2015
Hoch Lucile, Faure Helene, Roudaut Hermine, Schoenfelder Angele, Mann Andre, Girard Nicolas, Bihannic Laure, Ayrault Olivier, Petricci Elena, Taddei Maurizio, Rognan Didier, Ruat Martial
Abstract excerpt
The Smoothened (Smo) receptor, a member of class F G protein-coupled receptors, is the main transducer of the Hedgehog (Hh) signaling pathway implicated in a wide range of developmental and adult processes. Smo is the target of anticancer drugs that bind to a long and narrow cavity in the 7-transmembrane (7TM) domain. X-ray structures of human Smo (hSmo) bound to several ligands have revealed 2 types of...
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