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Cancer Cell. 2017 Jul 10;32(1):9-25. doi: 10.1016/j.ccell.2017.06.005.

Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology.

Author information

1
Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, UK. Electronic address: julian.blagg@icr.ac.uk.
2
Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, UK. Electronic address: paul.workman@icr.ac.uk.

Abstract

Small-molecule chemical probes or tools have become progressively more important in recent years as valuable reagents to investigate fundamental biological mechanisms and processes causing disease, including cancer. Chemical probes have also achieved greater prominence alongside complementary biological reagents for target validation in drug discovery. However, there is evidence of widespread continuing misuse and promulgation of poor-quality and insufficiently selective chemical probes, perpetuating a worrisome and misleading pollution of the scientific literature. We discuss current challenges with the selection and use of chemical probes, and suggest how biologists can and should be more discriminating in the probes they employ.

KEYWORDS:

PAINS; Pan-Assay Interference Compounds; biochemical selectivity; chemical probe; chemical reactivity; chemical tool; ligand promiscuity; lipophilicity; pharmacological audit trail; pharmacophore crossing; target validation

PMID:
28697345
PMCID:
PMC5511331
DOI:
10.1016/j.ccell.2017.06.005
[Indexed for MEDLINE]
Free PMC Article

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