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Therapeutic modulation of transcription factor activity
J G Emery1, E H Ohlstein, M Jaye
1Dept of Musculoskeletal Diseases, GlaxoSmithKline Pharmaceuticals, UW2109, King of Prussia, PA 19406-0939, USA.
Trends in Pharmacological Sciences
|May 8, 2001
Summary
Targeting transcription factors offers a new therapeutic strategy for diseases caused by aberrant gene expression. Advances in drug discovery now allow direct targeting of transcription factor complexes, moving beyond indirect modulation.
Area of Science:
- Molecular Biology
- Pharmacology
- Genetics
Background:
- Aberrant gene expression is a key driver of disease pathophysiology.
- Transcription factors regulate gene expression and are crucial therapeutic targets.
- Current drugs primarily modulate transcription factors indirectly via signaling pathways.
Purpose of the Study:
- To explore the potential of directly targeting transcription factor activity for therapeutic benefit.
- To highlight advancements in drug discovery enabling direct modulation of transcription factor complexes.
Main Methods:
- Review of current therapeutic strategies targeting transcription factors.
- Discussion of recent progress in high-throughput screening technologies for drug discovery.
Main Results:
- Transcription factor modulation is a promising therapeutic avenue.
- High-throughput screening can identify molecules targeting transcription factor complexes directly.
- Direct targeting circumvents indirect modulation pathways.
Conclusions:
- Directly targeting transcription factor complexes represents a significant advancement in drug discovery.
- This approach offers a more precise therapeutic strategy for diseases linked to aberrant gene expression.