Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0O0FB)
Name
Cytochrome P450 2J2 (CYP2J2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Albendazole monooxygenase (hydroxylating); Albendazole monooxygenase (sulfoxide-forming); Arachidonic acid epoxygenase; CYPIIJ2; Hydroperoxy icosatetraenoate isomerase
Family Lyase/isomerase/ligase (L/I/G)  >>  Intramolecular transferase (EC 5.4)
Organism
Homo sapiens (Human)
Gene Name CYP2J2 Gene ID
1573
UniProt ID CP2J2_HUMAN (click to find more protein-related data of this DBT)
INTEDE ID DME0031 (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
MLAAMGSLAAALWAVVHPRTLLLGTVAFLLAADFLKRRRPKNYPPGPWRLPFLGNFFLVD
FEQSHLEVQLFVKKYGNLFSLELGDISAVLITGLPLIKEALIHMDQNFGNRPVTPMREHI
FKKNGLIMSSGQAWKEQRRFTLTALRNFGLGKKSLEERIQEEAQHLTEAIKEENGQPFDP
HFKINNAVSNIICSITFGERFEYQDSWFQQLLKLLDEVTYLEASKTCQLYNVFPWIMKFL
PGPHQTLFSNWKKLKLFVSHMIDKHRKDWNPAETRDFIDAYLKEMSKHTGNPTSSFHEEN
LICSTLDLFFAGTETTSTTLRWALLYMALYPEIQEKVQAEIDRVIGQGQQPSTAARESMP
YTNAVIHEVQRMGNIIPLNVPREVTVDTTLAGYHLPKGTMILTNLTALHRDPTEWATPDT
FNPDHFLENGQFKKREAFMPFSIGKRACLGEQLARTELFIFFTSLMQKFTFRPPNNEKLS
LKFRMGITISPVSHRLCAVPQV
Function
A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) in the cardiovascular system. Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the epoxidation of double bonds of PUFA. Converts arachidonic acid to four regioisomeric epoxyeicosatrienoic acids (EpETrE).
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Glutamic acid hydrochloride 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
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 51 nM (estimated based on the structural similarity with CHEMBL575060 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID EAA3_HUMAN
          DIG Name: Antipyrine 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
Other agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 > 50000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP2J2_HUMAN
          DIG Name: Aspartic 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
Vaccine adjuvant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 19498.45 nM (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID EAA3_HUMAN
References
1 Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2. J Med Chem. 2008 Jul 24; 51(14):4085-92.
2 Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. Drug Metab Dispos. 2013 Jan; 41(1):60-71.
3 Chemoenzymatic Synthesis and Pharmacological Characterization of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid Transporter Inhibitors. J Med Chem. 2018 Sep 13; 61(17):7741-7753.

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