Cancer Cell
Volume 32, Issue 1, 10 July 2017, Pages 9-25
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Perspective
Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology

https://doi.org/10.1016/j.ccell.2017.06.005Get rights and content
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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

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

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