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Current opinion in chemical biology 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
JournalCurrent opinion in chemical biology
Volume14
Issue3
Pages331-40
Date Published2010/06/01
ISSN1367-5931
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.

URLhttp://linkinghub.elsevier.com/retrieve/pii/S1367-5931(10)00048-7
DOI10.1016/j.cbpa.2010.03.022
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/20395165?dopt=Abstract