Isocitrate Dehydrogenase Inhibitor

Isocitrate dehydrogenase inhibitors in acute myeloid leukemia - PMC

IDH inhibitors have shown good clinical response in AML patients. Hence, enasidenib and ivosidenib, the IDH2 and IDH1 inhibitors developed by Agios ...

Management of isocitrate dehydrogenase 1/2 mutated acute ...

Olutasidenib is a quinolone derived allosteric inhibitor of mutant IDH1 that binds to a hydrophobic pocket near the active site and stabilizes ...

Isocitrate Dehydrogenase-1 Inhibitors | DrugBank Online

Ivosidenib, An isocitrate dehydrogenase-1 inhibitor used to treat acute myeloid leukemia and cholangiocarcinoma in adults with a susceptible IDH1 mutation.

Isocitrate Dehydrogenase Inhibitor - an overview - ScienceDirect.com

IDH inhibitor treatment causes leukemic cells to release inflammatory cytokines, which further causes differentiation syndrome.

The regulatory mechanisms and inhibitors of isocitrate ...

Once the gain of function mutation occurs, the affinity between mutant IDH1 and substrate decreases, and the activity of IDH1WT is inhibited by forming ...

Isocitrate dehydrogenase inhibitors in acute myeloid leukemia

IDH inhibitors have shown good clinical response in AML patients. Based on phase 1/2 clinical trials, enasidenib and ivosidenib have been approved by the Food ...

Mutant Isocitrate Dehydrogenase 1 Inhibitor Ivosidenib in ...

Ivosidenib monotherapy induced durable remissions in patients with mIDH1 ND AML not eligible for IC (76% had secondary AML, 47% prior HMA ...

Isocitrate dehydrogenase-1 (IDH1) inhibitors | DrugBank Online

Ivosidenib, An isocitrate dehydrogenase-1 inhibitor used to treat acute myeloid leukemia and cholangiocarcinoma in adults with a susceptible IDH1 mutation.

Mutant Isocitrate Dehydrogenase Inhibitors as Targeted Cancer ...

In this review, we will summarize the molecular pathways and oncogenic consequences associated with mutIDH with a particular emphasis on glioma and AML.

Assessing inhibitors of mutant isocitrate dehydrogenase using a ...

Isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2) are key metabolic enzymes that are mutated in a variety of cancers to confer a ...

Isocitrate Dehydrogenase Inhibitor - an overview - ScienceDirect.com

Isocitrate dehydrogenases (IDH) are essential metabolic enzymes in the tricarboxylic acid (TCA) cycle involved with catalyzing the conversion of isocitrate to ...

Isocitrate Dehydrogenase (IDH) - MedchemExpress.com

Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) ...

Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 ...

Here we present the discovery and biochemical characterization of two novel inhibitors of wild-type IDH1.

Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate ...

Isocitrate dehydrogenase (IDH) 1/2 gain-of-function variants catalyze the production of the oncometabolite 2-hydroxyglutarate and are validated ...

Isoform Switching as a Mechanism of Acquired Resistance to Mutant ...

... Isocitrate Dehydrogenase Inhibition ... Differentiation syndrome associated with enasidenib, a selective inhibitor of mutant isocitrate dehydrogenase 2: analysis ...

Differentiation Syndrome Associated With Enasidenib, a Selective ...

Importance Enasidenib mesylate, a mutant isocitrate dehydrogenase 2 (IDH2) protein inhibitor that promotes differentiation of leukemic ...

Isocitrate Dehydrogenase (IDH) Inhibitors, Agonists and Modulators

Isocitrate Dehydrogenase inhibitors alter the activity of IDH enzymes, resulting in reduction of α-ketoglutarate to D-2-hydroxyglutarate, a competitive ...

Isocitrate Dehydrogenase Inhibitors in Glioma: From Bench to Bedside

IDH inhibitors are becoming increasingly a part of clinical practice in neuro-oncology. Initial results of the phase III clinical trial with vorasidenib are ...

Isocitrate dehydrogenase mutations in gliomas: A review of current ...

Ivosidenib is a specific, reversible, allosteric competitive inhibitor of mutant IDH1, and has shown moderate blood–brain barrier penetration ...

Clinical Implications of Isocitrate Dehydrogenase Mutations ... - MDPI

Another mechanism of resistance to mIDH inhibitors is the formation of secondary IDH mutations. FDA-approved mIDH inhibitors inhibit mutant enzymes through ...