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Curr Opin Chem Biol DOI:10.1016/j.cbpa.2010.03.022

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

Publication TypeJournal Article
Year of Publication2010
AuthorsKoehler, AN
JournalCurr Opin Chem Biol
Date Published2010 Jun
KeywordsDrug Delivery Systems, Drug Discovery, Humans, Oncogene Proteins, Fusion, Pharmaceutical Preparations, Receptors, Cytoplasmic and Nuclear, Transcription Factors

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.


Alternate JournalCurr Opin Chem Biol
PubMed ID20395165
PubMed Central IDPMC3248789
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