Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTDTWV0)

• DTT Name: Isocitrate dehydrogenase (IDH)
• Synonyms: Isocitrate dehydrogenase [NAD]
• Gene Name: IDH1
• DTT Type: Successful target; [1]
• BioChemical Class: CH-OH donor oxidoreductase
• UniProt ID: IDHC_HUMAN ; IDHP_HUMAN ; IDH3A_HUMAN ; IDH3B_HUMAN ; IDH3G_HUMAN
• TTD ID: T20808
• Sequence:
  MSKKISGGSVVEMQGDEMTRIIWELIKEKLIFPYVELDLHSYDLGIENRDATNDQVTKDA
  AEAIKKHNVGVKCATITPDEKRVEEFKLKQMWKSPNGTIRNILGGTVFREAIICKNIPRL
  VSGWVKPIIIGRHAYGDQYRATDFVVPGPGKVEITYTPSDGTQKVTYLVHNFEEGGGVAM
  GMYNQDKSIEDFAHSSFQMALSKGWPLYLSTKNTILKKYDGRFKDIFQEIYDKQYKSQFE
  AQKIWYEHRLIDDMVAQAMKSEGGFIWACKNYDGDVQSDSVAQGYGSLGMMTSVLVCPDG
  KTVEAEAAHGTVTRHYRMYQKGQETSTNPIASIFAWTRGLAHRAKLDNNKELAFFANALE
  EVSIETIEAGFMTKDLAACIKGLPNVQRSDYLNTFEFMDKLGENLKIKLAQAKL
• Function: It may tightly associate or interact with the pyruvate dehydrogenase complex. Plays a role in intermediary metabolism and energy production.
• KEGG Pathway:
  Citrate cycle (TCA cycle) (hsa00020)
  Glutathione metabolism (hsa00480)
  Metabolic pathways (hsa01100)
  Biosynthesis of antibiotics (hsa01130)
  Carbon metabolism (hsa01200)
  2-Oxocarboxylic acid metabolism (hsa01210)
  Biosynthesis of amino acids (hsa01230)
  Peroxisome (hsa04146)
• Reactome Pathway:
  NADPH regeneration (R-HSA-389542)
  Neutrophil degranulation (R-HSA-6798695)
  Peroxisomal protein import (R-HSA-9033241)
  Nuclear events mediated by NFE2L2 (R-HSA-9759194)
  Abnormal conversion of 2-oxoglutarate to 2-hydroxyglutarate (R-HSA-2978092)
• BioCyc Pathway: MetaCyc:HS06502-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ENASIDENIB MESYLATE	DMPOU5H	Acute myeloid leukaemia	2A60	Approved	[1]

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AG-221	DMS0ZBI	Acute myelogenous leukaemia	2A41	Phase 3	[2]
AG-881	DMIE1WY	Glioma	2A00.0	Phase 3	[3]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Acute myelocytic leukaemia	2C82	Bone marrow	6.06E-02	0.11	0.24

References

• [1] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [2] New Developments in the Pathogenesis and Therapeutic Targeting of the IDH1 Mutation in Glioma. Int J Med Sci. 2015; 12(3): 201-213.
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)