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NADP isocitrate dehydrogenase 2 (isocitrate dehydrogenase [NADP] mitochondrial)

Function: - catalyzes reversable conversion of isocitrate to 2-oxoglutarate - role in intermediary metabolism & energy production - may tightly associate or interact with pyruvate dehydrogenase complex isocitrate + NADP+ 2-oxoglutarate + CO2 + NADPH Cofactor: - binds 1 Mg+2 or Mn+2 per subunit Structure: - homodimer - belongs to the isocitrate & isopropylmalate dehydrogenases family Compartment: mitochondria Laboratory: - IDH2 gene mutation Pharmacology: - IDH2 inhibitor enasidenib (Idhifa) FDA-approved for treatment of refactory acute myeloid leukemia (AML) with IDH2 gene mutation - apparently IDH2 promotes cell growth of AML myelobasts - vorasidenib (Servier) inhibits mutant IDH2 investigational treatment of gliomas with IDH2 gene mutation

General

metalloprotein mitochondrial protein NADP isocitrate dehydrogenase

Properties

SIZE: entity length = 452 aa MW = 51 kD COMPARTMENT: mitochondria MOTIF: cofactor-binding site [115-117] COFACTOR-BOUND: NADP MOTIF: binding site SITE: 117-117 FOR-BINDING-OF: Substrate cofactor-binding site [122-122] COFACTOR-BOUND: NADP Substrate binding {134-140} binding site SITE: 149-149 FOR-BINDING-OF: Substrate binding site SITE: 172-172 FOR-BINDING-OF: Substrate tyrosine residue {179} lysine residue {251} manganese [Mn]-binding site SITE: 291-291 cofactor-binding site [299-299] COFACTOR-BOUND: NADP manganese [Mn]-binding site SITE: 314-314 cofactor-binding site [349-354] COFACTOR-BOUND: NADP cofactor-binding site [367-367] COFACTOR-BOUND: NADP

Database Correlations

OMIM 147650 UniProt P48735 Pfam PF00180 Kegg hsa:3418 ENZYME 1.1.1.42

References

  1. UniProt :accession O75874
  2. FDA News Release. August 1, 2017 FDA approves new targeted treatment for relapsed or refractory acute myeloid leukemia. https://www.fda.gov/newsevents/newsroom/pressannouncements/ucm569421.htm