Tchem CYP2C8 Cytochrome P450 2C8

Protein Summary

Description

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme responsible for the metabolism the anti-cancer drug paclitaxel (taxol). This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and its expression is induced by phenobarbital. The enzyme is known to metabolize many xenobiotics, including the anticonvulsive drug mephenytoin, benzo(a)pyrene, 7-ethyoxycoumarin, and the anti-cancer drug taxol. This gene is located within a cluster of cytochrome P450 genes on chromosome 10q24. Several transcript variants encoding a few different isoforms have been found for this gene. [provided by RefSeq, Nov 2010]

Uniprot Accession IDs

• P10632
• A8K9N8
• B0AZN2
• B7Z1F6
• Q5VX93
• Q8WWB1
• Q9UCZ9

Gene Name

• CYP2C8

Ensembl ID

• ENST00000371270
• ENSP00000360317
• ENSG00000138115
• ENST00000535898
• ENSP00000445062

Symbol

• CPC8
• CYPIIC8
• CYP2C8DM
• MP-12/MP-20

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
drug	1
chemical	0.97
disease	0.83
biological term	0.82
molecular function	0.81

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 373.47   (req: < 5)

Gene RIFs: 121   (req: <= 3)

Antibodies: 200   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 373.47   (req: >= 5)

Gene RIFs: 121   (req: > 3)

Antibodies: 200   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 20

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 5

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 1

Approved Drugs (1)

Explore Approved Drugs

1 – 1 of 1

phenelzine

CYP2C8Tchem

Ki: 5.13999987

Active Ligands (5)

Explore Active Ligands

1 – 5 of 5

CHEMBL2036213

CYP2C8Tchem

IC50: 7.36999989

CHEMBL3910478

CYP2C8Tchem

IC50: 6.3

CHEMBL3925961

CYP2C8Tchem

IC50: 6.52

CHEMBL3911035

CYP2C8Tchem

IC50: 6.05

CHEMBL3969750

CYP2C8Tchem

IC50: 6.52

Protein Data Bank (5)

1 – 5 of 5

PDB Structure Id	Ligand	Method	Resolution (Å)	M.W. (kDa)	Pub Year	Title

PDB Structure Id	M.W.	Resolution	Pub Year

Pathways (30)

Reactome (15)

KEGG (7)

PathwayCommons (1)

WikiPathways (7)

Arachidonic acid metabolism (R-HSA-2142753)

Click on a row in the table to change the structure displayed.

Items per page:

5

1 – 5 of 15

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Arachidonic acid metabolism	59 targets	R-HSA-2142753
Reactome	Biological oxidations	221 targets	R-HSA-211859
Reactome	Biosynthesis of DHA-derived SPMs	17 targets	R-HSA-9018677
Reactome	Biosynthesis of maresin-like SPMs	6 targets	R-HSA-9027307
Reactome	Biosynthesis of maresins	8 targets	R-HSA-9018682

Name	Explore in Pharos	Explore in Source
Arachidonic acid metabolism	59 targets	R-HSA-2142753
Biological oxidations	221 targets	R-HSA-211859
Biosynthesis of DHA-derived SPMs	17 targets	R-HSA-9018677
Biosynthesis of maresin-like SPMs	6 targets	R-HSA-9027307
Biosynthesis of maresins	8 targets	R-HSA-9018682

Gene Ontology Terms (24)

Functions (9)

Components (4)

Processes (11)

Items per page:

10

1 – 9 of 9

GO Term	Evidence	Assigned by
caffeine oxidase activity	Inferred from Direct Assay (IDA)	BHF-UCL
estrogen 16-alpha-hydroxylase activity	Inferred from Direct Assay (IDA)	BHF-UCL
monooxygenase activity	Inferred from Direct Assay (IDA)	BHF-UCL
arachidonic acid epoxygenase activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
heme binding	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
steroid hydroxylase activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
aromatase activity	Inferred from Electronic Annotation (IEA)	UniProtKB-EC
iron ion binding	Inferred from Electronic Annotation (IEA)	InterPro

Protein-Protein Interactions (132)

Explore Interacting Targets

1 – 10 of 132

• See Interactions on String-DB

EPHX1

Tchem

Family: Enzyme

Novelty: 0.00210581

Score: 0.949

Data Source: STRINGDB

EPHX2

Tchem

Family: Enzyme

Novelty: 0.00298106

Score: 0.949

Data Source: STRINGDB

CYP3A4

Tclin

Family: Enzyme

Novelty: 0.00020884

Score: 0.948

Data Source: STRINGDB

CYP4A11

Tbio

Novelty: 0.01325821

Score: 0.944

Data Source: STRINGDB

CYP4F2

Tchem

Family: Enzyme

Novelty: 0.00647783

Score: 0.937

Data Source: STRINGDB

CYP4F3

Tbio

Family: Enzyme

Novelty: 0.01901093

Score: 0.933

Data Source: STRINGDB

PTGS2

Tclin

Family: Enzyme

Novelty: 0.00008134

Score: 0.93

Data Source: STRINGDB

CYP1A2

Tchem

Novelty: 0.00045419

Score: 0.928

Data Source: STRINGDB

CYP4F8

Tbio

Novelty: 0.09383843

Score: 0.926

Data Source: STRINGDB

CYP1A1

Tchem

Novelty: 0.00028982

Score: 0.924

Data Source: STRINGDB

Publication Statistics

PubMed Score  373.47

PubMed score by year

Reset Zoom

PubTator Score  435.9

PubTator score by year

Reset Zoom

Amino Acid Sequence

Residue Counts

Sequence

MEPFVVLVLCLSFMLLFSLWRQSCRRRKLPPGPTPLPIIGNMLQIDVKDICKSFTNFSKVYGPVFTVYFG

1-70

MNPIVVFHGYEAVKEALIDNGEEFSGRGNSPISQRITKGLGIISSNGKRWKEIRRFSLTTLRNFGMGKRS

70-140

IEDRVQEEAHCLVEELRKTKASPCDPTFILGCAPCNVICSVVFQKRFDYKDQNFLTLMKRFNENFRILNS

140-210

PWIQVCNNFPLLIDCFPGTHNKVLKNVALTRSYIREKVKEHQASLDVNNPRDFIDCFLIKMEQEKDNQKS

210-280

EFNIENLVGTVADLFVAGTETTSTTLRYGLLLLLKHPEVTAKVQEEIDHVIGRHRSPCMQDRSHMPYTDA

280-350

VVHEIQRYSDLVPTGVPHAVTTDTKFRNYLIPKGTTIMALLTSVLHDDKEFPNPNIFDPGHFLDKNGNFK

350-420

KSDYFMPFSAGKRICAGEGLARMELFLFLTTILQNFNLKSVDDLKNLNTTAVTKGIVSLPPSYQICFIPV

420-490

MEPFVVLVLCLSFMLLFSLWRQSCRRRKLPPGPTPLPIIGNMLQIDVKDICKSFTNFSKVYGPVFTVYFGMNPIVVFHGYEAVKEALIDNGEEFSGRGNSPISQRITKGLGIISSNGKRWKEIRRFSLTTLRNFGMGKRSIEDRVQEEAHCLVEELRKTKASPCDPTFILGCAPCNVICSVVFQKRFDYKDQNFLTLMKRFNENFRILNSPWIQVCNNFPLLIDCFPGTHNKVLKNVALTRSYIREKVKEHQASLDVNNPRDFIDCFLIKMEQEKDNQKSEFNIENLVGTVADLFVAGTETTSTTLRYGLLLLLKHPEVTAKVQEEIDHVIGRHRSPCMQDRSHMPYTDAVVHEIQRYSDLVPTGVPHAVTTDTKFRNYLIPKGTTIMALLTSVLHDDKEFPNPNIFDPGHFLDKNGNFKKSDYFMPFSAGKRICAGEGLARMELFLFLTTILQNFNLKSVDDLKNLNTTAVTKGIVSLPPSYQICFIPV

Find similar targets by:

Uniprot Keyword

3D-structure
Alternative splicing
Complete proteome
Direct protein sequencing
Endoplasmic reticulum
Heme
Iron
Membrane
Metal-binding
Microsome