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egl-9 family hypoxia inducible factor 2

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Target id: 2832

Nomenclature: egl-9 family hypoxia inducible factor 2

Abbreviated Name: PHD1

Family: Prolyl hydroxylases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 407 19q13.2 EGLN2 egl-9 family hypoxia inducible factor 2
Mouse - 419 7 15.83 cM Egln2 egl-9 family hypoxia-inducible factor 2
Rat - 415 1q21 Egln2 egl-9 family hypoxia-inducible factor 2
Gene and Protein Information Comments
Using alternative methionine initiation codons, two isoforms of human EGLN2 have been reported , generating PHD1p40 (374 amino acids; UniProt identifier Q96KS0-2) and PHD1p43 (407 amino acids; UniProt identifier Q96KS0-1). PHD1p43 is considered the canonocal protein.
Previous and Unofficial Names Click here for help
HIF prolyl hydroxylase 1 | HIFPH1 | egl-9 family hypoxia-inducible factor 2
Database Links Click here for help
Alphafold Q96KS0 (Hs), Q91YE2 (Mm), Q6AYU4 (Rn)
BRENDA 1.14.11.29
ChEMBL Target CHEMBL3028 (Hs)
Ensembl Gene ENSG00000269858 (Hs), ENSMUSG00000058709 (Mm), ENSRNOG00000020947 (Rn)
Entrez Gene 112398 (Hs), 112406 (Mm), 308457 (Rn)
Human Protein Atlas ENSG00000269858 (Hs)
KEGG Enzyme 1.14.11.29
KEGG Gene hsa:112398 (Hs), mmu:112406 (Mm), rno:308457 (Rn)
OMIM 606424 (Hs)
Pharos Q96KS0 (Hs)
RefSeq Nucleotide NM_080732 (Hs), NM_053046 (Hs), NM_053208 (Mm), NM_001004083 (Rn)
RefSeq Protein NP_542770 (Hs), NP_444274 (Hs), NP_444438 (Mm), NP_001004083 (Rn)
UniProtKB Q96KS0 (Hs), Q91YE2 (Mm), Q6AYU4 (Rn)
Wikipedia EGLN2 (Hs)
Enzyme Reaction Click here for help
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 Value Parameter Reference
compound 6ee [PMID: 22364528] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.7 pIC50 3
⤷ pIC50 9.7 (IC50 2x10-10 M) [3]
roxadustat Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition - - 2
⤷ [2]
molidustat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition - - 2
⤷ [2]
vadadustat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition - - 2
⤷ [2]
desidustat Small molecule or natural product Hs Inhibition - - 1
⤷ [1]

References

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1. Desai RC, Pandaya V, Patel PR. (2014) Novel quinolone derivatives. Patent number: WO2014102818A1. Assignee: Cadila Healthcare Limited. Priority date: 24/12/2012. Publication date: 03/07/2014.

2. Joharapurkar AA, Pandya VB, Patel VJ, Desai RC, Jain MR. (2018) Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. J Med Chem, 61 (16): 6964-6982. [PMID:29712435]

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

Prolyl hydroxylases: egl-9 family hypoxia inducible factor 2. Last modified on 05/12/2022. Accessed on 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2832.