3 years ago

A Bioinorganic Approach to Fragment-Based Drug Discovery Targeting Metalloenzymes

A Bioinorganic Approach to Fragment-Based Drug Discovery Targeting Metalloenzymes
Seth M. Cohen
Metal-dependent enzymes (i.e., metalloenzymes) make up a large fraction of all enzymes and are critically important in a wide range of biological processes, including DNA modification, protein homeostasis, antibiotic resistance, and many others. Consequently, metalloenzymes represent a vast and largely untapped space for drug development. The discovery of effective therapeutics that target metalloenzymes lies squarely at the interface of bioinorganic and medicinal chemistry and requires expertise, methods, and strategies from both fields to mount an effective campaign. In this Account, our research program that brings together the principles and methods of bioinorganic and medicinal chemistry are described, in an effort to bridge the gap between these fields and address an important class of medicinal targets.

Publisher URL: http://dx.doi.org/10.1021/acs.accounts.7b00242

DOI: 10.1021/acs.accounts.7b00242

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