Drugging Fuzzy Complexes in Transcription
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fmolb-08-795743.pdf
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1.16 MB
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Unknown
Checksum (MD5)
cdd2bed22de7470f09ea72966d8586f1
Author(s)
Su, Bonnie G.
Henley, Matthew J.
Date Issued
December 2021
Publisher
Frontiers Media SA
Citation
Su, Bonnie G. and Henley, Matthew J. 2021. "Drugging Fuzzy Complexes in Transcription." 8.
Version
Final published version
Abstract
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.
MIT Department
Koch Institute for Integrative Cancer Research at MIT
Broad Institute of MIT and Harvard
Massachusetts Institute of Technology. Department of Biology
Terms of Use
Creative Commons Attribution 4.0 International license
Persistent DSpace Link
DOI of Published Version
https://doi.org/10.3389/fmolb.2021.795743
