85753-15-7Relevant academic research and scientific papers
Colocalization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor
Zhou, Fang,Ding, Kang,Zhou, Yiqing,Liu, Yang,Liu, Xiaoyan,Zhao, Fei,Wu, Yiran,Zhang, Xianjun,Tan, Qiwen,Xu, Fei,Tan, Wenfu,Xiao, Youli,Zhao, Suwen,Tao, Houchao
, p. 9983 - 9989 (2019)
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, πinteractions, 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.
CALCIUM ION CHANNEL MODULATORS and USES THEREOF
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Page/Page column 87, (2010/04/27)
Compounds of formula (I), wherein R1 is hydrogen, hydroxyl or aralkyl; R2 is an optionally substituted alkyl, aryl or heteroaryl (said substituents are selected from hydroxyl, alkoxyl, haloalkoxyl, aryl, heteroaryl, cycloalkyl, amino, monoalkylamino, dialkylamino, alkylsulphonyl, alkylsulphinyl, alkylsulphonylamino, acylamino, saturated or partially unsaturated heterocyclic groups and groups of formula COY); W is selected from oxygen, sulphur, groups of formula NR7, wherein R7 is hydrogen, alkyl, aryl or heteroaryl and groups of formula CR8R9, wherein R8 and R9 are hydrogen, alkyl, aryl or heteroaryl; and X is selected from nitrogen and groups of formula CR10, wherein R10 is hydrogen, alkyl, aryl, heteroaryl, halogen or haloalkyl, inhibit the interaction between Cavx channels and Cavβ proteins and are of use in the treatment and prevention of a number of diseases and conditions including pain and lower urinary tract disorders.
