Article
1-BENZYLSPIRO[PIPERIDINE-4,1'-PYRIDO[3,4-b]indole] 'co-potentiators' for minimal function CFTR mutants.
European journal of medicinal chemistry - 1 Jan 2021
Son Jung-Ho, Phuan Puay-Wah, Zhu Jie S, Lipman Elena, Cheung Amy, Tsui Ka Yi, Tantillo Dean J, Verkman Alan S, Haggie Peter M, Kurth Mark J
Abstract excerpt
We previously identified a spiro [piperidine-4,1-pyrido [3,4-b]indole] class of co-potentiators that function in synergy with existing CFTR potentiators such as VX-770 or GLGP1837 to restore channel activity of a defined subset of minimal function cystic fibrosis transmembrane conductance regulator (CFTR) mutants. Here, structure-activity studies were conducted to improve their potency over the previously...
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