Approximately 10% of currently prescribed drugs directly target the nuclear receptor class of transcription factors. Examples include tamoxifen and bicalutamide for the treatment of breast and prostate cancer, respectively, and various types of anti-inflammatory and anabolic steroids. In addition, transcription factors are often indirectly modulated by drugs through signaling cascades. It might be possible to directly target other less-explored transcription factors such as NF-κB with drugs. Transcription factors outside the nuclear receptor family are thought to be more difficult to target with small molecule therapeutics since it is not clear that they are “drugable” but progress has been made on Pax2 and the notch pathway.
Transcription Factors are proteins that regulate gene reading from DNA sequences
• A direct modulation of a Transcription Factor activity by small molecules can be achieved through
– Mimetics of peptide motifs that bind at either activation domain (AD) or signal-sensing domain (SSD)
– Mimetics of DNA motifs that bind at a DNA-binding domain (DBD)
• Transcription Factors are promising therapeutic targets for
– Oncology, e.g. immunological response modulators, tumor suppressors, oncogenes regulators
– Metabolic diseases, e.g. diabetes, osteoporosis, high-density lipoproteins (HDL) regulation
– Cardiovascular system, e.g. atherosclerosis, thrombosis
– Inflammation, e.g. autoimmune diseases, immune response suppression
A unique collection of small molecule compounds with annotated activities for Transcription Factors targets
❑ Annotated activities : 39 transcription factors targets
❑ Express Delivery : 480 compounds
❑ Complete Version : 5278 compounds
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