Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0L3YD)
Name
HIF-prolyl hydroxylase 2 (EGLN1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Hypoxia-inducible factor prolyl hydroxylase 2; C1orf12; Egl nine homolog 1; HIF-PH2; PHD2; HIF-prolyl hydroxylase 2; HPH-2; Prolyl hydroxylase domain-containing protein 2; SM-20
Family Oxidoreductase (ORase)  >>  Oxygen paired donor oxidoreductase (EC 1.14)
Organism
Homo sapiens (Human)
Gene Name EGLN1 Gene ID
54583
UniProt ID EGLN1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T32880 (click to find more therapeutic target data of this DBT)
INTEDE ID DME0462 (click to find more drug-metabolizing enzyme data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MANDSGGPGGPSPSERDRQYCELCGKMENLLRCSRCRSSFYCCKEHQRQDWKKHKLVCQG
SEGALGHGVGPHQHSGPAPPAAVPPPRAGAREPRKAAARRDNASGDAAKGKVKAKPPADP
AAAASPCRAAAGGQGSAVAAEAEPGKEEPPARSSLFQEKANLYPPSNTPGDALSPGGGLR
PNGQTKPLPALKLALEYIVPCMNKHGICVVDDFLGKETGQQIGDEVRALHDTGKFTDGQL
VSQKSDSSKDIRGDKITWIEGKEPGCETIGLLMSSMDDLIRHCNGKLGSYKINGRTKAMV
ACYPGNGTGYVRHVDNPNGDGRCVTCIYYLNKDWDAKVSGGILRIFPEGKAQFADIEPKF
DRLLFFWSDRRNPHEVQPAYATRYAITVWYFDADERARAKVKYLTGEKGVRVELNKPSDS
VGKDVF
Function
Cellular oxygen sensor that catalyzes, under normoxic conditions, the post-translational formation of 4-hydroxyproline in hypoxia-inducible factor (HIF) alpha proteins. Hydroxylates a specific proline found in each of the oxygen-dependent degradation (ODD) domains (N-terminal, NODD, and C-terminal, CODD) of HIF1A. Also hydroxylates HIF2A. Has a preference for the CODD site for both HIF1A and HIF1B. Hydroxylated HIFs are then targeted for proteasomal degradation via the von Hippel-Lindau ubiquitination complex.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Fumaric acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Acidulant; Antioxidant; Complexing agent; Flavoring agent; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 19000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID EGLN1_HUMAN
          DIG Name: Succinic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Buffering agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 3000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID EGLN1_HUMAN
References
1 Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. J Med Chem. 2008 Nov 27; 51(22):7053-6.

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