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New technology overcomes the most difficult drug-forming cancer gene, from dream to reality

2021-07-06 16:54:58 JE Read

RAS (KRAS, NRAS and HRAS), the most common family of mutated genes in tumors, and the first human oncogene to be identified, are classified as KRAS, NRAS and HRAS, and were discovered by Robert Weinberg in 1982.

As the most common oncogene in human tumors, mutations in RAS genes encode RAS proteins that block the conversion of GTP to GDP, leading to constitutive activation of RAF kinases in cells. pathways. These signaling pathways have important roles in promoting cell survival, proliferation and cytokine release.

The most common tumors with RAS gene mutations are: pancreatic cancer (97.7%), colorectal cancer (52.2%), myeloma (42.6%), and lung adenocarcinoma (30.9%). However, such an important and widespread RAS gene mutation, after more than three decades of research, still has not found effective drugs for RAS targets, because RAS inhibitors are difficult to develop, because, RAS has also been labeled as non-drugable.

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Just recently, a team of researchers at the University of Leeds, however, discovered the weakness of this mutant protein, which brings hope for the development of new powerful drugs. Among other things, the University of Leeds researchers have taken advantage of the Institute of Molecular and Cellular Biology's own proprietary mimetic biotechnology platform to pinpoint drug-ready "pockets" in the protein for effective treatment.

The researchers believe that this fact has allowed them to demonstrate that mimetic technology can have such a dramatic impact and deliver significant benefits when it comes to treating challenging pathologies. We have identified small molecules that bind to the RAS, so it will be an exciting process over the next few years to explore these small molecules and thus develop efficacious drugs.

It is worth noting that many cutting-edge therapies targeting RAS drugs in different directions are currently in the early stages of preclinical and clinical trials. For example, Amgen presented top-line data from its phase I clinical trial of its KRAS inhibitor AMG510 at the 2019 ASCO Annual Meeting. And, Amgen again announced the latest development progress of AMG510 at WCLC 2019. The data showed that AMG510 produced good efficacy, safety and tolerability in targeting NSCLC patients carrying KRAS G12C mutation.

It is foreseeable that continued breakthroughs in research efforts on new approaches to tackle RAS will not only accelerate new drug development, but also help drug developers screen matched subject populations in clinical trials, provide patients with the safety and efficacy of specific therapeutic agents, help screen patients for possible benefits, and improve treatment outcomes and reduce healthcare costs.