Targeting K-Ras Mutations Show Promise Towards Ending Ras’s “Undruggable” Era

Title:Targeting K-Ras Mutations Show Promise Towards Ending Ras’s “Undruggable” Era

Volume: 29 Issue: 12

Author(s): Paul D. Adams*Djamali Muhoza

Affiliation:

• Department of Chemistry and Biochemistry, University of Arkansas at Fayetteville, 72701, Arkansas, AR 72701, USA

Keywords: Ras, Drug targets, Small molecule inhibitor, effectors

Abstract: It has almost been 40 years since the Ras proteins were discovered as the first human oncogenes. They remain among the most important genes for regulating mammalian cell growth and are involved in more than a quarter of human cancers. Out of 167 members of the Ras superfamily, KRas mutations are the most abundant in human cancers. Particularly, the K-Ras G12C mutations are known to be involved in pancreatic, colon and lung cancers as well as leukemias. Though progress has been made, approaches targeting Ras proteins for therapeutic purposes remain challenging. No drugs treating Ras-related cancers are currently on the market. However, there is now renewed interest in the Ras area, and newer approaches have highlighted the targeting of several types of tumors and treating cancer patients. This review will summarize recent K-Ras drug candidates and approaches in the preclinical, clinical and post-clinical pipelines that show promise for targeting and reducing Ras-related tumors. Macromolecules such as mRNA vaccines, siRNA, and T-cell receptors that target Ras will also be discussed. The newer molecules and the recent approaches to be discussed suggest that the “undruggable” era of Ras proteins could be coming to an end.

Cite this article as:

Adams D. Paul*, Muhoza Djamali, Targeting K-Ras Mutations Show Promise Towards Ending Ras’s “Undruggable” Era, Protein & Peptide Letters 2022; 29 (12) . https://dx.doi.org/10.2174/0929866529666221003124202

DOI https://dx.doi.org/10.2174/0929866529666221003124202	Print ISSN 0929-8665
Publisher Name Bentham Science Publisher	Online ISSN 1875-5305