Document Report Card

Basic Information

ID: ALA4414554

Journal: J Med Chem

Title: Colocalization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor.

Authors: Zhou F, Ding K, Zhou Y, Liu Y, Liu X, Zhao F, Wu Y, Zhang X, Tan Q, Xu F, Tan W, Xiao Y, Zhao S, Tao H.

Abstract: We unveiled an underside binding site on smoothened receptor (SMO) by a colocalization strategy using two structurally complementary photoaffinity probes derived from a known ligand Allo-1. Docking study and structural dissection identified key interactions within the site, including hydrogen bonding, π-π interactions, and hydrophobic interactions between Allo-1 and its contacting residues. Taken together, our results reveal the molecular base of Allo-1 binding and provide a basis for the design of new-generation ligands to overcome drug resistance.

CiteXplore: 31408335

DOI: 10.1021/acs.jmedchem.9b00283