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Public resources for chemical probes: the journey so far and the road ahead.

Authors
  • Antolin, Albert A1, 2, 3
  • Workman, Paul2, 3
  • Al-Lazikani, Bissan1, 2, 3
  • 1 The Department of Data Science, The Institute of Cancer Research, London, SM2 5NG, UK.
  • 2 CRUK Cancer Therapeutics Unit, The Institute of Cancer Research, London, SM2 5NG, UK.
  • 3 CRUK ICR/Imperial Convergence Science Centre, London, SM2 5NG, UK.
Type
Published Article
Journal
Future Medicinal Chemistry
Publisher
"Future Science, LTD"
Publication Date
Apr 01, 2021
Volume
13
Issue
8
Pages
731–747
Identifiers
DOI: 10.4155/fmc-2019-0231
PMID: 31778323
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

High-quality small molecule chemical probes are extremely valuable for biological research and target validation. However, frequent use of flawed small-molecule inhibitors produces misleading results and diminishes the robustness of biomedical research. Several public resources are available to facilitate assessment and selection of better chemical probes for specific protein targets. Here, we review chemical probe resources, discuss their current strengths and limitations, and make recommendations for further improvements. Expert review resources provide in-depth analysis but currently cover only a limited portion of the liganded proteome. Computational resources encompass more proteins and are regularly updated, but have limitations in data availability and curation. We show how biomedical scientists may use these resources to choose the best available chemical probes for their research.

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