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Curr Opin Chem Biol. 2010 Jun;14(3):331-40. doi: 10.1016/j.cbpa.2010.03.022. Epub 2010 Apr 13.

A complex task? Direct modulation of transcription factors with small molecules.

Author information

1
Broad Institute of Harvard and MIT, Chemical Biology Program, 7 Cambridge Center, Cambridge, MA 02142, USA. koehler@broadinstitute.org

Abstract

Transcription factors with aberrant activity in disease are promising yet untested targets for therapeutic development, particularly in oncology. Directly inhibiting or activating the function of a transcription factor requires specific disruption or recruitment of protein-protein or protein-DNA interactions. The discovery or design of small molecules that specifically modulate these interactions has thus far proven to be a significant challenge and the protein class is often perceived to be 'undruggable.' This review will summarize recent progress in the development of small-molecule probes of transcription factors and provide evidence to challenge the notion that this important protein class is chemically intractable.

PMID:
20395165
PMCID:
PMC3248789
DOI:
10.1016/j.cbpa.2010.03.022
[Indexed for MEDLINE]
Free PMC Article

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