Drugging Fuzzy Complexes in Transcription
Author(s)
Su, Bonnie G.; Henley, Matthew J.
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Transcription factors (TFs) are one of the most promising but underutilized classes of drug targets. The high degree of intrinsic disorder in both the structure and the interactions (i.e., “fuzziness”) of TFs is one of the most important challenges to be addressed in this context. Here, we discuss the impacts of fuzziness on transcription factor drug discovery, describing how disorder poses fundamental problems to the typical drug design, and screening approaches used for other classes of proteins such as receptors or enzymes. We then speculate on ways modern biophysical and chemical biology approaches could synergize to overcome many of these challenges by directly addressing the challenges imposed by TF disorder and fuzziness.
Date issued
2021-12Department
Koch Institute for Integrative Cancer Research at MIT; Broad Institute of MIT and Harvard; Massachusetts Institute of Technology. Department of BiologyPublisher
Frontiers Media SA
Citation
Su, Bonnie G. and Henley, Matthew J. 2021. "Drugging Fuzzy Complexes in Transcription." 8.
Version: Final published version
ISSN
2296-889X