Application of Fragment Screening and Merging to the Discovery of Inhibitors of the Mycobacterium tuberculosis Cytochrome P450 CYP121

Sean A. Hudson, Kirsty J. McLean, Sachin Surade, Yong Qing Yang, David Leys, Alessio Ciulli, Andrew W. Munro, Chris Abell

Research output: Contribution to journalArticle

51 Citations (Scopus)

Abstract

Pieces of the puzzle: The first fragment-based approach was used to target cytochrome P450 enzymes (CYPs) for drug development (see scheme). The experiments provide new insights into the binding site of the essential Mycobacterium tuberculosis CYP121 enzyme, and resulted in a promising novel lead compound based on fragment merging.

Original languageEnglish
Pages (from-to)9311-9316
Number of pages6
JournalAngewandte Chemie - International Edition
Volume51
Issue number37
Early online date13 Aug 2012
DOIs
Publication statusPublished - 10 Sep 2012
Externally publishedYes

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