期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 54, 期 46, 页码 13516-13537出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201504357
关键词
cancer; drug design; inhibitors; proteins; small GTPases
资金
- Studienstiftung des deutschen Volkes
- Fonds der Chemischen Industrie
- German Research Foundation (DFG)
- AstraZeneca
- Bayer CropScience
- Bayer HealthCare
- Boehringer Ingelheim
- Merck KGaA
- Max Planck Society
- Deutschen Forschungsgemeinschaft [SFB 642]
- German Research Foundation (Emmy Noether program) [GR3592/2-1]
Small GTPases are a family of GDP-/GTP-binding proteins that serve as biomolecular switches inside cells to control a variety of essential cellular processes. Aberrant function and regulation of small GTPases is associated with a variety of human diseases, thus rendering these proteins highly interesting targets in drug discovery. However, this class of proteins has been considered undruggable, as intensive decade-long efforts did not yield clinically relevant direct modulators of small GTPases. Recently, the targeting of small GTPases has gained fresh impetus through the discovery of novel transient cavities on the protein surfaces and the application of new targeting strategies. Besides Ras proteins, other small GTPases have attracted increased attention since improved biological insight in combination with novel targeting strategies identified them as promising targets in drug discovery. This Review gives an overview of relevant aspects of the superfamily of small GTPases and summarizes recent progress and perspectives for the direct modulation of these challenging targets.
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