Substrate Fragmentation for the Design ofM. tuberculosisCYP121 Inhibitors
Abstract
The cyclo-dipeptide substrates of the essential M. tuberculosis (Mtb) enzyme CYP121 were deconstructed into their component fragments and screened against the enzyme. A number of hits were identified, one of which exhibited an unexpected inhibitor-like binding mode. The inhibitory pharmacophore was elucidated, and fragment binding affinity was rapidly improved by synthetic elaboration guided by the structures of CYP121 substrates. The resulting...
Paper Details
Title
Substrate Fragmentation for the Design ofM. tuberculosisCYP121 Inhibitors
Published Date
Jul 19, 2016
Journal
Volume
11
Issue
17
Pages
1924 - 1935
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