Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous <i>MTAP</i> Deletion
Zenon Konteatis, Jeremy Travins, Stefan Größ, Katya Marjon, Amelia Barnett, Everton Mandley, Brandon Nicolay, Raj Nagaraja, Yue Chen, Yabo Sun, Zhixiao Liu, Jie Yu, Zhixiong Ye, Fan Jiang, Wentao Wei, Fang Cheng, Yi Gao, Peter Kalev, Marc L. Hyer, Byron DeLaBarre, Lei Jin, Anil K. Padyana, Lenny Dang, Joshua Murtie, Scott A. Biller, Zhihua Sui, Kevin M. Marks
Abstract
into current clinical studies (ClinicalTrials.gov NCT03435250).
Topics & Concepts
Methionine AdenosyltransferaseChemistryCDKN2AAllosteric regulationEnzymeCancer researchPotencyMethionineSmall moleculeKinaseCancerBiochemistryIn vitroGeneBiologyGeneticsAmino acidCancer-related gene regulationEpigenetics and DNA MethylationRNA modifications and cancer