Journal
CURRENT OPINION IN CHEMICAL BIOLOGY
Volume 14, Issue 3, Pages 331-340Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.cbpa.2010.03.022
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Funding
- US National Cancer Institute's Initiative for Chemical Genetics [N01-CO-12400]
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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.
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