General Information of Target

Target ID LDTP12267
Target Name Cytochrome P450 4F12 (CYP4F12)
Gene Name CYP4F12
Gene ID 66002
Synonyms
Cytochrome P450 4F12; EC 1.14.14.1; CYPIVF12
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAASRLDFGEVETFLDRHPELFEDYLMRKGKQEMVEKWLQRHSQGQGALGPRPSLAGTSS
LAHSTCRGGSSVGGGTGPNGSAHSQPLPGGGDCGGVPLSPSWAGGSRGDGNLQRRASQKE
LRKSFARSKAIHVNRTYDEQVTSRAQEPLSSVRRRALLRKASSLPPTTAHILSALLESRV
NLPRYPPTAIDYKCHLKKHNERQFFLELVKDISNDLDLTSLSYKILIFVCLMVDADRCSL
FLVEGAAAGKKTLVSKFFDVHAGTPLLPCSSTENSNEVQVPWGKGIIGYVGEHGETVNIP
DAYQDRRFNDEIDKLTGYKTKSLLCMPIRSSDGEIIGVAQAINKIPEGAPFTEDDEKVMQ
MYLPFCGIAISNAQLFAASRKEYERSRALLEVVNDLFEEQTDLEKIVKKIMHRAQTLLKC
ERCSVLLLEDIESPVVKFTKSFELMSPKCSADAENSFKESMEKSSYSDWLINNSIAELVA
STGLPVNISDAYQDPRFDAEADQISGFHIRSVLCVPIWNSNHQIIGVAQVLNRLDGKPFD
DADQRLFEAFVIFCGLGINNTIMYDQVKKSWAKQSVALDVLSYHATCSKAEVDKFKAANI
PLVSELAIDDIHFDDFSLDVDAMITAALRMFMELGMVQKFKIDYETLCRWLLTVRKNYRM
VLYHNWRHAFNVCQLMFAMLTTAGFQDILTEVEILAVIVGCLCHDLDHRGTNNAFQAKSG
SALAQLYGTSATLEHHHFNHAVMILQSEGHNIFANLSSKEYSDLMQLLKQSILATDLTLY
FERRTEFFELVSKGEYDWNIKNHRDIFRSMLMTACDLGAVTKPWEISRQVAELVTSEFFE
QGDRERLELKLTPSAIFDRNRKDELPRLQLEWIDSICMPLYQALVKVNVKLKPMLDSVAT
NRSKWEELHQKRLLASTASSSPASVMVAKEDRN
Target Bioclass
Enzyme
Family
Cytochrome P450 family
Subcellular location
Endoplasmic reticulum membrane
Function
A cytochrome P450 monooxygenase involved in the metabolism of endogenous polyunsaturated fatty acids (PUFAs). 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 (CPR; NADPH-ferrihemoprotein reductase). Catalyzes the hydroxylation of carbon hydrogen bonds, with preference for omega-2 position. Metabolizes (5Z,8Z,11Z,14Z)-eicosatetraenoic acid (arachidonate) toward 18-hydroxy arachidonate. Catalyzes the epoxidation of double bonds of PUFAs such as docosapentaenoic and docosahexaenoic acids. Has low omega-hydroxylase activity toward leukotriene B4 and arachidonate. Involved in the metabolism of xenobiotics. Catalyzes the hydroxylation of the antihistamine drug ebastine.
Uniprot ID
Q9HCS2
Ensemble ID
ENST00000324632.10
HGNC ID
HGNC:18857
ChEMBL ID
CHEMBL3509589

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CORL23 SNV: p.L228F .
HT SNV: p.S314P .
KMCH1 SNV: p.R365L .
MELHO Deletion: p.D142_K143del
SNV: p.W144G
.
MEWO SNV: p.P396S .
MFE319 SNV: p.G328R .
NCIH2170 SNV: p.M80I DBIA    Probe Info 
REH SNV: p.A182T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IPM
 Probe Info 
C50(0.00); C401(0.00); C402(0.00)  LDD0241  [1]
DBIA
 Probe Info 
C50(2.53); C468(1.25)  LDD3321  [2]
WYneN
 Probe Info 
N.A.  LDD0021  [3]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
AEA-DA
 Probe Info 
2.42  LDD0146  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0082  FK866 A-549 2.42  LDD0146  [4]
 LDCM0022  KB02 A498 C50(1.30)  LDD2259  [2]
 LDCM0023  KB03 A498 C50(2.31)  LDD2676  [2]
 LDCM0024  KB05 SH4 C50(2.53); C468(1.25)  LDD3321  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Complex I assembly factor TIMMDC1, mitochondrial (TIMMDC1) Tim17/Tim22/Tim23 family Q9NPL8

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ketoconazole Small molecular drug DB01026
Ponesimod Small molecular drug DB12016

References

1 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
4 A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045.