isocitrate dehydrogenase (NADP(+)) 1, cytosolic

Target id: 2884

Nomenclature: isocitrate dehydrogenase (NADP(+)) 1, cytosolic

Systematic Nomenclature: IDH1

Family: 1.1.1.42 Isocitrate dehydrogenases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for isocitrate dehydrogenase (NADP(+)) 1, cytosolic in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 414 2q33.3 IDH1 isocitrate dehydrogenase (NADP(+)) 1, cytosolic
Mouse - 414 1 C2 Idh1 isocitrate dehydrogenase 1 (NADP+)
Rat - 414 9q32 Idh1 isocitrate dehydrogenase (NADP(+)) 1
Previous and Unofficial Names
isocitrate dehydrogenase 1 (NADP+), soluble | isocitrate dehydrogenase [NADP] cytoplasmic | isocitrate dehydrogenase 1 (NADP) | isocitrate dehydrogenase 1 (NADP+)
Database Links
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ChEMBL Target
Ensembl Gene
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GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
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KEGG Gene
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RefSeq Nucleotide
RefSeq Protein
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Enzyme Reaction
EC Number: 1.1.1.42 Isocitrate + NADP(+) <=> 2-oxoglutarate + CO2 + NADPH
Description Reaction Reference
Isocitrate + NADP+ <=> 2-oxoglutarate + CO2 + NADPH

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
AGI-5198 Hs Inhibition 4.9 pKi
pKi 4.9 (Ki 1.3x10-5 M)
ivosidenib Hs Inhibition - - 1
[1]
Inhibitor Comments
The two ligands against this target are hihgly selective for mutant IDH1 isoforms and have low activity against wild type enzyme.
Clinically-Relevant Mutations and Pathophysiology
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Missense Human R132C, R132G, R132S, R132H, R132L 394C>T, 394C>G, 394C>A, 395G>A, 395G>T IDH1 mutations associated with cancers such as glioma and some hematological malignancies. 2-3
Clinically-Relevant Mutations and Pathophysiology Comments
The majority (80-90%) of IDH1 mutations in glioma are R132H. IDH1 is mutated in the majority of lower grade diffuse gliomas (grades II-III) and also in most secondary glioblastomas. It is rare in newly diagnosed glioblastoma.

References

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1. Lemieux RM, Popovici-Muller J, Travins J, Cai Z, Cui D, Zhou D. (2013) Therapeutically active compounds and their methods of use. Patent number: WO2013107291. Assignee: Agios Pharmaceuticals, Inc.. Priority date: 19/01/2012. Publication date: 25/07/2013.

2. Rohle D, Popovici-Muller J, Palaskas N, Turcan S, Grommes C, Campos C, Tsoi J, Clark O, Oldrini B, Komisopoulou E et al.. (2013) An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science340 (6132): 626-30. [PMID:23558169]

3. Walter MJ, Shen D, Shao J, Ding L, White BS, Kandoth C, Miller CA, Niu B, McLellan MD, Dees ND et al.. (2013) Clonal diversity of recurrently mutated genes in myelodysplastic syndromes. Leukemia27 (6): 1275-82. [PMID:23443460]

How to cite this page

1.1.1.42 Isocitrate dehydrogenases: isocitrate dehydrogenase (NADP(+)) 1, cytosolic. Last modified on 20/07/2016. Accessed on 11/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2884.