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Enzyme inhibitor discovery by activity-based protein profiling

Academic Article
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Overview

authors

  • Niphakis, M. J.
  • Cravatt, Benjamin

publication date

  • 2014

journal

  • Annual Review of Biochemistry  Journal

abstract

  • Eukaryotic and prokaryotic organisms possess huge numbers of uncharacterized enzymes. Selective inhibitors offer powerful probes for assigning functions to enzymes in native biological systems. Here, we discuss how the chemical proteomic platform activity-based protein profiling (ABPP) can be implemented to discover selective and in vivo-active inhibitors for enzymes. We further describe how these inhibitors have been used to delineate the biochemical and cellular functions of enzymes, leading to the discovery of metabolic and signaling pathways that make important contributions to human physiology and disease. These studies demonstrate the value of selective chemical probes as drivers of biological inquiry.

subject areas

  • Animals
  • Binding, Competitive
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical
  • Drug Design
  • Drug Discovery
  • Enzyme Inhibitors
  • Gene Expression Profiling
  • Humans
  • Lactones
  • Phenotype
  • Photochemistry
  • Proteome
  • Proteomics
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Research

keywords

  • activity-based protein profiling
  • chemical proteomics
  • enzyme
  • inhibitor
  • target engagement
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Identity

International Standard Serial Number (ISSN)

  • 0066-4154

Digital Object Identifier (DOI)

  • 10.1146/annurev-biochem-060713-035708

PubMed ID

  • 24905785
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Additional Document Info

start page

  • 341

end page

  • 377

volume

  • 83

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