A complex task? Direct modulation of transcription factors with small molecules
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 int...
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| Veröffentlicht in: | Current opinion in chemical biology 2010-06, Vol.14 (3), p.331-340 |
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| container_title | Current opinion in chemical biology |
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| creator | Koehler, Angela N |
| description | 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. |
| doi_str_mv | 10.1016/j.cbpa.2010.03.022 |
| format | Article |
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| identifier | ISSN: 1367-5931 |
| ispartof | Current opinion in chemical biology, 2010-06, Vol.14 (3), p.331-340 |
| issn | 1367-5931 1879-0402 1879-0402 |
| language | eng |
| recordid | cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_3248789 |
| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Drug Delivery Systems Drug Discovery - methods Humans Oncogene Proteins, Fusion - antagonists & inhibitors Pharmaceutical Preparations - chemistry Receptors, Cytoplasmic and Nuclear - antagonists & inhibitors Transcription Factors - chemistry Transcription Factors - metabolism |
| title | A complex task? Direct modulation of transcription factors with small molecules |
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