Article
A Pan-RAS Inhibitor with a Unique Mechanism of Action Blocks Tumor Growth and Induces Antitumor Immunity in Gastrointestinal Cancer.
Cancer research - 3 Mar 2025
Foote Jeremy B, Mattox Tyler E, Keeton Adam B, Chen Xi, Smith Forrest T, Berry Kristy, Holmes Thomas W, Wang Junwei, Huang Chung-Hui, Ward Antonio, Mitra Amit K, Ramirez-Alcantara Veronica, Hardy Cherlene, Fleten Karianne G, Flatmark Kjersti, Yoon Karina J, Sarvesh Sujith, Nagaraju Ganji P, Bandi Dhana Sekhar Reddy, Maxuitenko Yulia Y, Valiyaveettil Jacob, Carstens Julienne L, Buchsbaum Donald J, Yang Jennifer, Zhou Gang, Nurmemmedov Elmar, Babic Ivan, Gaponeko Vadim, Abdelkarim Hazem, Boyd Michael R, Gorman Greg, Manne Upender, Bae Sejong, El-Rayes Bassel F, Piazza Gary A
Abstract excerpt
Activated RAS is a common driver of cancer that was considered undruggable for decades. Recent advances have enabled the development of RAS inhibitors, but the efficacy of these inhibitors remains limited by resistance. In this study, we developed a pan-RAS inhibitor, ADT-007, (Z)-2-(5-fluoro-1-(4-hydroxy-3,5-dimethoxybenzylidene)-2-methyl-1H-inden-3-yl)-N-(furan-2-ylmethyl)acetamide, that binds nucleotide-free...
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