The DOI matches its Crossref record; 146 of the 146 references it cites were found in a registry or an index.
Probing the Probes: Fitness Factors For Small Molecule Tools
Open accessAbstract
Chemical probes for interrogating biological processes are of considerable current interest. Cell permeable small molecule tools have a major role in facilitating the functional annotation of the human genome, understanding both physiological and pathological processes, and validating new molecular targets. To be valuable, chemical tools must satisfy necessary criteria and recent publications have suggested objective guidelines for what makes a useful chemical probe. Although recognizing that such guidelines may be valuable, we caution against overly restrictive rules that may stifle innovation in favor of a "fit-for-purpose" approach. Reviewing the literature and providing examples from the cancer field, we recommend a series of "fitness factors" to be considered when assessing chemical probes. We hope this will encourage innovative chemical biology research while minimizing the generation of poor quality and misleading biological data, thus increasing understanding of the particular biological area, to the benefit of basic research and drug discovery.
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Cites
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The Essential Medicinal Chemistry of Curcumin
Nelson, K. M., Dahlin, J. L., Bisson, J., Graham, J., Pauli, G. F., & Walters, M. A. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b00975 · Cited by 1,956
Hsp90 Molecular Chaperone Inhibitors: Are We There Yet?
Neckers, L., & Workman, P. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-11-1000 · Cited by 891
Self-citationThe promise and peril of chemical probes
Arrowsmith, C. H., Audia, J. E., Austin, C., Baell, J., Bennett, J., Blagg, J., Bountra, C., Brennan, P. E., Brown, P. J., Bunnage, M. E., et al. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1867 · Cited by 839
Self-citationLeverson, J. D., Zhang, H., Chen, J., Tahir, S. K., Phillips, D. C., Xue, J., Nimmer, P., Jin, S., Smith, M., Xiao, Y., et al. (2015) · Cell Death & Disease · doi:10.1038/cddis.2014.561 · Cited by 440
Comprehensive characterization of the Published Kinase Inhibitor Set
Elkins, J. M., Fedele, V., Szklarz, M., Abdul Azeez, K. R., Salah, E., Mikolajczyk, J., Romanov, S., Sepetov, N., Huang, X.-P., Roth, B. L., et al. (2016) · Nature Biotechnology · doi:10.1038/nbt.3374 · Cited by 323
Metadata
- Authors
- Workman, P., & Collins, I.
- Venue
- Chemistry & Biology
- Publisher
- Elsevier BV
- Published
- 2010-06
- Volume
- 17
- Issue
- 6
- Pages
- 561-577
- ISSN
- 1074-5521 (ISSN-L)
- OpenAlex
- W2166594615
- Cited by
- 299
- References
- 146
- FWCI
- 20.08
- Type
- journal article
- Language
- en
- Open access
- hybrid
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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