egl-9 family hypoxia inducible factor 1

Target id: 2833

Nomenclature: egl-9 family hypoxia inducible factor 1

Abbreviated Name: PHD2

Family: 1.14.11.29 2-oxoglutarate oxygenases

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 egl-9 family hypoxia inducible factor 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 426 1q42.1 EGLN1 egl-9 family hypoxia inducible factor 1
Mouse - 400 8 E2 Egln1 egl-9 family hypoxia-inducible factor 1
Rat - 338 19q12 Egln1 egl-9 family hypoxia-inducible factor 1
Previous and Unofficial Names
EGL nine (C.elegans) homolog 1 | HIF prolyl hydroxylase 2 | HIFPH2 | SM-20 | ZMYND6 | egl-9 family hypoxia-inducible factor 1
Database Links
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 1.14.11.29

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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
compound 6ee [PMID: 22364528] Hs Inhibition 9.7 pIC50 3
pIC50 9.7 (IC50 2x10-10 M) [3]
IOX2 Hs Inhibition 7.7 pIC50 1
pIC50 7.7 (IC50 2.2x10-8 M) [1]
IOX1 Hs Inhibition 4.5 pIC50 2
pIC50 4.5 (IC50 3.3x10-5 M) [2]
Clinically-Relevant Mutations and Pathophysiology
Disease:  Erythrocytosis, familial, 3; ECYT3
Synonyms: Autosomal dominant secondary polycythemia [Orphanet: ORPHA247511]
OMIM: 609820
Orphanet: ORPHA247511

References

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1. Chowdhury R, Candela-Lena JI, Chan MC, Greenald DJ, Yeoh KK, Tian YM, McDonough MA, Tumber A, Rose NR, Conejo-Garcia A et al.. (2013) Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases. ACS Chem. Biol., 8 (7): 1488-96. [PMID:23683440]

2. Schiller R, Scozzafava G, Tumber A, Wickens JR, Bush JT, Rai G, Lejeune C, Choi H, Yeh TL, Chan MC et al.. (2014) A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem, 9 (3): 566-71. [PMID:24504543]

3. Vachal P, Miao S, Pierce JM, Guiadeen D, Colandrea VJ, Wyvratt MJ, Salowe SP, Sonatore LM, Milligan JA, Hajdu R et al.. (2012) 1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia. J. Med. Chem., 55 (7): 2945-59. [PMID:22364528]

How to cite this page

1.14.11.29 2-oxoglutarate oxygenases: egl-9 family hypoxia inducible factor 1. Last modified on 17/07/2017. Accessed on 20/06/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2833.