4.7 Editorial Material

Spotlight on Accessory Proteins: RTK-RAS-MAPK Modulators as New Therapeutic Targets

期刊

BIOMOLECULES
卷 11, 期 6, 页码 -

出版社

MDPI
DOI: 10.3390/biom11060895

关键词

adaptor proteins; anchoring proteins; docking proteins; KRAS; scaffold proteins; RAF kinase; RTK; MEK; ERK

资金

  1. Research Committee of the Medical Faculty of the Heinrich Heine University Dusseldorf [2020-70/9772617]
  2. German Research Foundation (Deutsche Forschungsgemeinschaft or DFG) [AH 92/8-1, IRTG 1902-p6]
  3. European Network on Noonan Syndrome and Related Disorders (NSEuroNet) [01GM1621B]
  4. German Federal Ministry of Education and Research (BMBF)German Network of RASopathy Research (GeNeRARe) [01GM1902C]

向作者/读者索取更多资源

The RTK-RAS-MAPK axis is extensively studied and related to cancer and RASopathies. However, directly targeting this cascade is still insufficient due to issues like drug toxicity, resistance, and low efficacy. Significant progress has been made in understanding the spatiotemporal features of the axis's constituent members, with many of these modulators emerging as potential therapeutic targets.
The RTK-RAS-MAPK axis is one of the most extensively studied signaling cascades and is related to the development of both cancers and RASopathies. In the last 30 years, many ideas and approaches have emerged for directly targeting constituent members of this cascade, predominantly in the context of cancer treatment. These approaches are still insufficient due to undesirable drug toxicity, resistance, and low efficacy. Significant advances have been made in understanding the spatiotemporal features of the constituent members of the RTK-RAS-MAPK axis, which are linked and modulated by many accessory proteins. Given that the majority of such modulators are now emerging as attractive therapeutic targets, a very small number of accessory inhibitors have yet to be discovered.

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