Drugs for ‘Protein Clouds’: Targeting Intrinsically Disordered Transcription Factors
Document Type
Article
Publication Date
2010
Digital Object Identifier (DOI)
https://doi.org/10.1016/j.coph.2010.09.005
Abstract
Transcription factors (TFs) are very attractive but difficult drug targets. The difficulties come from several directions including the binding promiscuity of TFs and the intrinsically disordered nature of their binding sites, which often resemble ‘protein clouds’. For a long time the targeting of proteins without defined structures was considered infeasible. Data have now emerged showing that selective blocking of specific interactions of intrinsically disordered TFs with their protein binding partners is possible. Initial hits have been optimized to increase their specificity and affinity. Several strategies have been elaborated for elucidating the mechanisms of blocking of intrinsic disorder-based protein–protein interactions. However, challenges remain in the field of drug development for ‘protein clouds’; such development is still in its earliest stage.
Was this content written or created while at USF?
Yes
Citation / Publisher Attribution
Current Opinion in Pharmacology, v. 10, issue 6, p. 782-788
Scholar Commons Citation
Dunker, A. Keith and Uversky, Vladimir N., "Drugs for ‘Protein Clouds’: Targeting Intrinsically Disordered Transcription Factors" (2010). Molecular Medicine Faculty Publications. 473.
https://digitalcommons.usf.edu/mme_facpub/473
