A complex task? Direct modulation of transcription factors with small molecules.
Curr Opin Chem Biol
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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
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Journal | Curr Opin Chem Biol
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Volume | 14
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Issue | 3
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Pages | 331-40
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Date Published | 2010 Jun
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ISSN | 1879-0402
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URL | |
DOI | 10.1016/j.cbpa.2010.03.022
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PubMed ID | 20395165
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PubMed Central ID | PMC3248789
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Grant list | -C0-012400 / PHS HHS / United States
N01 / HL / NHLBI NIH HHS / United States
N01-C0-012400 / CO / NCI NIH HHS / United States
N01CO12400 / CA / NCI NIH HHS / United States
N01-CO-12400 / CO / NCI NIH HHS / United States
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