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The IDH enzyme catalyzes the oxidative carboxylation of isocitrate to α-ketoglutarate in the citric acid cycle, producing NADPH. Cancer-associated mutations in IDH1 and IDH2 result in the ...
The research team, led by Jing Chen, PhD, professor of medicine, discovered that AML cells are able to modify mutant IDH2 and regulate its activity, thus controlling the amount of 2-HG that it can ...
The study is published in an article in the journal Molecular Cell, titled, “Lysine acetylation restricts mutant IDH2 activity to optimize transformation in AML cells.” Financial support for ...
we were also able to demonstrate promising clinical activity, including multiple complete remissions, in patients whose blood cancers carried an IDH2 mutation, even at the lowest tested dose ...
To elucidate the relationship between mutant enzyme activity, 2-HG levels and oncogenic state, Agios developed a mutant-selective IDH2 inhibitor. Primary samples of acute myeloid leukemia (AML ...
Genomic analysis revealed BRAF F595L (variant allele frequency, 8.5%) and IDH2 R172W (8.3%) mutations. Fig 1. (A) Timeline of patient's diagnosis, treatment, and treatment responses. (B) In the MRI ...
The first patient received their first dose on May 11, 2024. HMPL-306 is a novel dual-inhibitor of IDH1 and IDH2 enzymes. Mutations of IDH1 and IDH2 have been implicated as drivers of certain ...
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