The DOI matches its Crossref record; 24 of the 24 references it cites were found in a registry or an index.
Drug Affinity Responsive Target Stability (DARTS) for Small-Molecule Target Identification
Open accessAbstract
Drug Affinity Responsive Target Stability (DARTS) is a relatively quick and straightforward approach to identify potential protein targets for small molecules. It relies on the protection against proteolysis conferred on the target protein by interaction with a small molecule. The greatest advantage of this method is being able to use the native small molecule without having to immobilize or modify it (e.g. by incorporation of biotin, fluorescent, radioisotope, or photo-affinity labels). Here we describe in detail the protocol for performing unbiased DARTS with complex protein lysate to identify potential binding targets of small molecules and for using DARTS-Western blotting to test, screen, or validate potential small molecule targets. Although the ideas have mainly been developed from studying molecules in areas of biology that are currently of interest to us and our collaborators, the general principles should be applicable to the analysis of all molecules in nature.
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Cites
Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay
Molina, D. M., Jafari, R., Ignatushchenko, M., Seki, T., Larsson, E. A., Dan, C., Sreekumar, L., Cao, Y., & Nordlund, P. (2013) · Science · doi:10.1126/science.1233606 · Cited by 2,261
Target identification using drug affinity responsive target stability (DARTS)
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Self-citationGeiger, T., Wehner, A., Schaab, C., Cox, J., & Mann, M. (2012) · Molecular & Cellular Proteomics · doi:10.1074/mcp.m111.014050 · Cited by 797
The metabolite α-ketoglutarate extends lifespan by inhibiting ATP synthase and TOR
Chin, R. M., Fu, X., Pai, M. Y., Vergnes, L., Hwang, H., Deng, G., Diep, S., Lomenick, B., Meli, V. S., Monsalve, G. C., et al. (2014) · Nature · doi:10.1038/nature13264 · Cited by 608
Self-citationTarget Identification for Small Bioactive Molecules: Finding the Needle in the Haystack
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Identification of Direct Protein Targets of Small Molecules
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Self-citationRask-Andersen, M., Masuram, S., & Schiöth, H. B. (2014) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev-pharmtox-011613-135943 · Cited by 282
Target Identification Using Drug Affinity Responsive Target Stability (DARTS)
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Metadata
- Authors
- Pai, M. Y., Lomenick, B., Hwang, H., Schiestl, R., McBride, W., Loo, J. A., & Huang, J.
- Venue
- Methods in Molecular Biology
- Publisher
- Springer New York
- Published
- 2014-12-22
- Volume
- 1263
- Pages
- 287-298
- ISSN
- 1064-3745 (ISSN-L)
- 1940-6029
- OpenAlex
- W90330895
- Cited by
- 354
- References
- 24
- FWCI
- 66.75
- Type
- book chapter
- Language
- en
- Open access
- green
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- Pai, M. Y., Lomenick, B., Hwang, H., Schiestl, R., McBride, W., Loo, J. A., & Huang, J. (2015). Drug Affinity Responsive Target Stability (DARTS) for Small-Molecule Target Identification. Methods in Molecular Biology. https://doi.org/10.1007/978-1-4939-2269-7_22
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