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A complex task? Direct modulation of transcription factors with small molecules.
|Publication Type||Journal Article|
|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.|
|Year of Publication||2010|
|Journal||Current opinion in chemical biology|
|Date Published (YYYY/MM/DD)||2010/06/01|