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Redefining the TGR5 Triterpenoid Binding Pocket at the C‐3 Position
Author(s) -
Genet Cédric,
Schmidt Céline,
Strehle Axelle,
Schoonjans Kristina,
Auwerx Johan,
Saladin Régis,
Wagner Alain
Publication year - 2010
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201000329
Subject(s) - triterpenoid , chemistry , stereochemistry , binding pocket , position (finance) , binding site , biochemistry , business , finance
A defining characteristic: Syntheses of potent TGR5 agonists were used to characterize binding interactions. A serie of C‐3 modified betulinic acid derivatives were synthesized and evaluated. Among them, epoxide 15 showed nanomolar activity.