Past and Future Strategies to Inhibit Membrane Localization of the KRAS Oncogene

International Journal of Molecular Sciences

Malak Haidar¹  Patrick Jacquemin¹ 

[1] De Duve Institute, Université Catholique de Louvain, 1200 Brussels, Belgium;

关键词: RAS;    KRAS;    plasma membrane;    cancer;   

DOI  :  10.3390/ijms222413193

来源: DOAJ

【 摘 要 】

KRAS is one of the most studied oncogenes. It is well known that KRAS undergoes post-translational modifications at its C-terminal end. These modifications are essential for its membrane location and activity. Despite significant efforts made in the past three decades to target the mechanisms involved in its membrane localization, no therapies have been approved and taken into the clinic. However, many studies have recently reintroduced interest in the development of KRAS inhibitors, either by directly targeting KRAS or indirectly through the inhibition of critical steps involved in post-translational KRAS modifications. In this review, we summarize the approaches that have been applied over the years to inhibit the membrane localization of KRAS in cancer and propose a new anti-KRAS strategy that could be used in clinic.

【 授权许可】

Unknown