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A complex task? Direct modulation of transcription factors with small molecules.
| Publication Type | Journal Article |
| Authors | Koehler, AN |
| 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 |
| Volume | 14 |
| Issue | 3 |
| Pages | 331-40 |
| Date Published (YYYY/MM/DD) | 2010/06/01 |
| ISSN Number | 1367-5931 |
| DOI | 10.1016/j.cbpa.2010.03.022 |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/20395165?dopt=Abstract |
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