Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous

Authors :: Zenon, Konteatis
Jeremy, Travins
Stefan, Gross
Katya, Marjon
Amelia, Barnett
Everton, Mandley
Brandon, Nicolay
Raj, Nagaraja
Yue, Chen
Yabo, Sun
Zhixiao, Liu
Jie, Yu
Zhixiong, Ye
Fan, Jiang
Wentao, Wei
Cheng, Fang
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
Source :: Journal of medicinal chemistry. 64(8)
Publication Year :: 2021
Abstract: The metabolic enzyme methionine adenosyltransferase 2A (MAT2A) was recently implicated as a synthetic lethal target in cancers with deletion of the methylthioadenosine phosphorylase (

Subjects :: S-Adenosylmethionine
Structure-Activity Relationship
Binding Sites
Purine-Nucleoside Phosphorylase
Drug Design
Neoplasms
Homozygote
Humans
Methionine Adenosyltransferase
Enzyme Inhibitors
Molecular Dynamics Simulation
Crystallography, X-Ray

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