Proteins > Isocitrate dehydrogenase [NADP] cytoplasmic
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Isocitrate dehydrogenase [NADP] cytoplasmic
An isocitrate dehydrogenase [NADP] cytoplasmic that is encoded in the genome of human. [PRO:DNx]
Synonyms
IDH;
EC 1.1.1.42;
Cytosolic NADP-isocitrate dehydrogenase;
IDP;
NADP(+)-specific ICDH;
Oxalosuccinate decarboxylase
Research
Bioassay Publications (18)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 13 (72.22) | 24.3611 |
| 2020's | 5 (27.78) | 2.80 |
Compounds (12)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| licochalcone a | Homo sapiens (human) | Kd | 21.8733 | 3 | 3 |
| nsc-287088 | Homo sapiens (human) | Kd | 45.3000 | 1 | 1 |
| SYC-435 | Homo sapiens (human) | EC50 | 2.4000 | 1 | 1 |
| agi-5198 | Homo sapiens (human) | EC50 | 0.0600 | 1 | 1 |
| ivosidenib | Homo sapiens (human) | EC50 | 0.0198 | 2 | 2 |
Design, synthesis and biological activity of 3-pyrazine-2-yl-oxazolidin-2-ones as novel, potent and selective inhibitors of mutant isocitrate dehydrogenase 1.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
Inhibition of cancer-associated mutant isocitrate dehydrogenases: synthesis, structure-activity relationship, and selective antitumor activity.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
Discovery of DC_H31 as potential mutant IDH1 inhibitor through NADPH-based high throughput screening.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
[no title available]Journal of natural products, , 11-22, Volume: 82, Issue:11, 2019
Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors.Bioorganic & medicinal chemistry, , 02-15, Volume: 27, Issue:4, 2019
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.Journal of medicinal chemistry, , 10-25, Volume: 61, Issue:20, 2018
Design, synthesis and biological evaluation of novel 5-hydroxy-2-methyl-4MedChemComm, , Mar-01, Volume: 9, Issue:3, 2018
Design, synthesis and biological activity of 3-pyrazine-2-yl-oxazolidin-2-ones as novel, potent and selective inhibitors of mutant isocitrate dehydrogenase 1.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1.ACS medicinal chemistry letters, , Oct-13, Volume: 7, Issue:10, 2016
Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.ACS medicinal chemistry letters, , Oct-11, Volume: 3, Issue:10, 2012
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Discovery and structure-activity-relationship study of novel conformationally restricted indane analogues for mutant isocitric dehydrogenase 1 (IDH1) inhibitors.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 27, Issue:23, 2017
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.ACS medicinal chemistry letters, , Feb-13, Volume: 11, Issue:2, 2020
Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
Enables
This protein enables 8 target(s):
| Target | Category | Definition |
|---|
| magnesium ion binding | molecular function | Binding to a magnesium (Mg) ion. [GOC:ai] |
| isocitrate dehydrogenase (NADP+) activity | molecular function | Catalysis of the reaction: isocitrate + NADP+ = 2-oxoglutarate + CO2 + NADPH. [RHEA:19629] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| cadherin binding | molecular function | Binding to cadherin, a type I membrane protein involved in cell adhesion. [GOC:bf] |
| NADP binding | molecular function | Binding to nicotinamide-adenine dinucleotide phosphate, a coenzyme involved in many redox and biosynthetic reactions; binding may be to either the oxidized form, NADP+, or the reduced form, NADPH. [GOC:ai] |
| NAD binding | molecular function | Binding to nicotinamide adenine dinucleotide, a coenzyme involved in many redox and biosynthetic reactions; binding may be to either the oxidized form, NAD+, or the reduced form, NADH. [GOC:ai] |
Located In
This protein is located in 9 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| peroxisome | cellular component | A small organelle enclosed by a single membrane, and found in most eukaryotic cells. Contains peroxidases and other enzymes involved in a variety of metabolic processes including free radical detoxification, lipid catabolism and biosynthesis, and hydrogen peroxide metabolism. [GOC:pm, PMID:9302272, UniProtKB-KW:KW-0576] |
| peroxisomal matrix | cellular component | The volume contained within the membranes of a peroxisome; in many cells the matrix contains a crystalloid core largely composed of urate oxidase. [GOC:curators, ISBN:0815316194] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| secretory granule lumen | cellular component | The volume enclosed by the membrane of a secretory granule. [GOC:rph] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
| tertiary granule lumen | cellular component | Any membrane-enclosed lumen that is part of a tertiary granule. [GO_REF:0000064, GOC:TermGenie, PMID:23650620] |
| ficolin-1-rich granule lumen | cellular component | Any membrane-enclosed lumen that is part of a ficolin-1-rich granule. [GO_REF:0000064, GOC:TermGenie, PMID:23650620] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
| peroxisome | cellular component | A small organelle enclosed by a single membrane, and found in most eukaryotic cells. Contains peroxidases and other enzymes involved in a variety of metabolic processes including free radical detoxification, lipid catabolism and biosynthesis, and hydrogen peroxide metabolism. [GOC:pm, PMID:9302272, UniProtKB-KW:KW-0576] |
Involved In
This protein is involved in 11 target(s):
| Target | Category | Definition |
|---|
| glyoxylate cycle | biological process | A modification of the TCA cycle occurring in some plants and microorganisms, in which isocitrate is cleaved to glyoxylate and succinate. Glyoxylate can then react with acetyl-CoA to form malate. [ISBN:0198506732] |
| tricarboxylic acid cycle | biological process | A nearly universal metabolic pathway in which the acetyl group of acetyl coenzyme A is effectively oxidized to two CO2 and four pairs of electrons are transferred to coenzymes. The acetyl group combines with oxaloacetate to form citrate, which undergoes successive transformations to isocitrate, 2-oxoglutarate, succinyl-CoA, succinate, fumarate, malate, and oxaloacetate again, thus completing the cycle. In eukaryotes the tricarboxylic acid is confined to the mitochondria. See also glyoxylate cycle. [ISBN:0198506732] |
| isocitrate metabolic process | biological process | The chemical reactions and pathways involving isocitrate, the anion of isocitric acid, 1-hydroxy-1,2,3-propanetricarboxylic acid. Isocitrate is an important intermediate in the TCA cycle and the glycoxylate cycle. [ISBN:0198506732] |
| 2-oxoglutarate metabolic process | biological process | The chemical reactions and pathways involving oxoglutarate, the dianion of 2-oxoglutaric acid. It is a key constituent of the TCA cycle and a key intermediate in amino-acid metabolism. [ISBN:0198506732] |
| glutathione metabolic process | biological process | The chemical reactions and pathways involving glutathione, the tripeptide glutamylcysteinylglycine, which acts as a coenzyme for some enzymes and as an antioxidant in the protection of sulfhydryl groups in enzymes and other proteins; it has a specific role in the reduction of hydrogen peroxide (H2O2) and oxidized ascorbate, and it participates in the gamma-glutamyl cycle. [ISBN:0198506732] |
| response to oxidative stress | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, e.g. superoxide anions, hydrogen peroxide (H2O2), and hydroxyl radicals. [GOC:jl, PMID:12115731] |
| female gonad development | biological process | The process whose specific outcome is the progression of the female gonad over time, from its formation to the mature structure. [GOC:dph, GOC:jid, GOC:tb] |
| response to steroid hormone | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a steroid hormone stimulus. [GOC:go_curators] |
| regulation of phospholipid catabolic process | biological process | Any process that modulates the rate, frequency, or extent of phospholipid catabolism, the chemical reactions and pathways resulting in the breakdown of phospholipids, any lipid containing phosphoric acid as a mono- or diester. [GOC:BHF, GOC:dph, GOC:tb] |
| regulation of phospholipid biosynthetic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of phospholipids. [GOC:mah] |
| NADP metabolic process | biological process | The chemical reactions and pathways involving nicotinamide-adenine dinucleotide phosphate, a coenzyme involved in many redox and biosynthetic reactions; metabolism may be of either the oxidized form, NADP, or the reduced form, NADPH. [GOC:mah] |