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

作者：Koehler Angela N^*

来源：Current Opinion in Chemical Biology, 2010, 14(3): 331-340.

DOI：10.1016/j.cbpa.2010.03.022

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.

• 出版日期2010-6