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TargetEnzymes

Cytochrome P450 3A5

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
1
Compounds
1
Binding constants
1
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

CP3A5_HUMANCYP3A5Homo sapiens

Cytochrome P450 3A5

A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins10681376,11093772,12865317,2732228. 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 hydroxylation of carbon-hydrogen bonds10681376,11093772,12865317,2732228. Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E212865317. Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione2732228. Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA)10681376. Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance11093772. Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine2732228

Quoted from UniProt’s FUNCTION annotation for P20815 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
UGT1A40.9780.0450.9060.769
UGT1A80.9760.0450.9060.731
UGT1A60.9750.0450.9060.733
UGT1A10.9740.0450.9060.726
UGT1A70.9740.0450.9060.726
UGT2B70.9740.0450.9060.726
UGT1A100.9740.0450.9060.726
CYP1A10.9710.0760.9090.588
CYP2B60.9700.0760.9080.574
CYP3A70.9680.5560.9000.059

Where it sits in the cell

  • Cytosol
  • Vesiclesadditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Endoplasmic reticulum membrane · Microsome membrane

Expression by cell type

Single cell type RNA, the 8 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Enterocytes1,916 nCPM
  • Foveolar cells1,066.6 nCPM
  • Hepatocytes1,064 nCPM
  • Urothelial cells674.9 nCPM
  • Cholangiocytes647.1 nCPM
  • Colonocytes613.5 nCPM
  • Proximal tubule cells603.7 nCPM
  • Esophageal apical cells396.9 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • liver319.4 nTPM
  • intestine167.3 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 1

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Cytochrome P450 3A5EnzymesKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687735