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

• DOI: 10.1002/anie.201202544
• Publication Date: 2012-08-13T12:35:16Z
• Authors: Sean A. Hudson; Kirsty J. McLean; Sachin Surade; Yong‐Qing Yang; David Leys; Alessio Ciulli; Andrew W. Munro; Chris Abell
• Keywords: Fragment (logic)

Pieces of the puzzle: The first fragment-based approach was used to target cytochrome P450 enzymes (CYPs) for drug development (see scheme). experiments provide new insights into binding site essential Mycobacterium tuberculosis CYP121 enzyme, and resulted in a promising novel lead compound based on fragment merging. Detailed facts importance specialist readers are published as "Supporting Information". Such documents peer-reviewed, but not copy-edited or typeset. They made available submitted by authors. Please note: publisher is responsible content functionality any supporting information supplied Any queries (other than missing content) should be directed corresponding author article.