Ontology highlight
ABSTRACT:
SUBMITTER: Coffman KC
PROVIDER: S-EPMC4136667 | biostudies-literature | 2014 Aug
REPOSITORIES: biostudies-literature
Coffman Keith C KC Nguyen Huy H HH Phuan Puay-Wah PW Hudson Brandi M BM Yu Gui J GJ Bagdasarian Alex L AL Montgomery Deanna D Lodewyk Michael W MW Yang Baoxue B Yoo Choong L CL Verkman A S AS Tantillo Dean J DJ Kurth Mark J MJ
Journal of medicinal chemistry 20140725 15
Conformationally constrained bithiazoles were previously found to have improved efficacy over nonconstrained bithiazoles for correction of defective cellular processing of the ΔF508 mutant cystic fibrosis transmembrane conductance regulator (CFTR) protein. In this study, two sets of constrained bithiazoles were designed, synthesized, and tested in vitro using ΔF508-CFTR expressing epithelial cells. The SAR data demonstrated that modulating the constraining ring size between 7- versus 8-membered ...[more]