CYP3 family | Enzymes | IUPHAR/BPS Guide to PHARMACOLOGY

CYP3 family C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

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Enzymes

CYP3A4 C Show summary »« Hide summary More detailed page

Target Id

1337

Nomenclature

CYP3A4

Previous and unofficial names

Genes

CYP3A4 (Hs)

Ensembl ID

ENSG00000160868 (Hs)

UniProtKB AC

P08684 (Hs)

EC number

1.14.13.67

Quinine + NADPH + O₂ = 3-hydroxyquinine + NADP⁺ + H₂O₂

1.14.13.97

Taurochenodeoxycholate + NADPH + O₂ = taurohyocholate + NADP⁺ + H₂O
Lithocholate + NADPH + O₂ = hyodeoxycholate + NADP⁺ + H₂O

1.14.13.32

Albendazole + NADPH + O₂ = albendazole S-oxide + NADP⁺ + H₂

1.14.13.157

1,8-cineole + NADPH + O₂ = 2-exo-hydroxy-1,8-cineole + NADP⁺ + H₂O

Substrates

tamoxifen [1]

codeine [1]

atorvastatin [1]

diazepam [1]

erlotinib [1]

Products

4-hydroxy-tamoxifen [5]

4-hydroxy-tamoxifen quinone methide [5]

Inhibitors

ritonavir pK_i >7.0 [4]

Comment

Metabolises a vast range of xenobiotics, including antidepressants, benzodiazepines, calcium channel blockers, and chemotherapeutic agents. CYP3A4 catalyses the 25-hydroxylation of trihydroxycholestane in liver microsomes [3].

CYP3A5 Show summary »« Hide summary

Target Id

1338

Nomenclature

CYP3A5

Previous and unofficial names

cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 5 | cytochrome P450, family 3, subfamily A, polypeptide 5

Genes

CYP3A5 (Hs)

Ensembl ID

ENSG00000106258 (Hs)

UniProtKB AC

P20815 (Hs)

EC number

1.14.14.1

Inhibitors

ritonavir pK_i 6.9 [2]

CYP3A7 Show summary »« Hide summary

Target Id

1339

Nomenclature

CYP3A7

Previous and unofficial names

cytochrome P450, subfamily IIIA, polypeptide 7 | cytochrome P450, family 3, subfamily A, polypeptide 7

Genes

CYP3A7 (Hs)

Ensembl ID

ENSG00000160870 (Hs)

UniProtKB AC

P24462 (Hs)

EC number

1.14.14.1

CYP3A43 Show summary »« Hide summary

Target Id

1340

Nomenclature

CYP3A43

Previous and unofficial names

Cytochrome P450 3A43 | cytochrome P450, family 3, subfamily A, polypeptide 43

Genes

CYP3A43 (Hs)

Ensembl ID

ENSG00000021461 (Hs)

UniProtKB AC

Q9HB55 (Hs)

EC number

1.14.14.1

References

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1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed on 18/11/2014. Modified on 18/11/2014. http://medicine.iupui.edu/clinpharm/ddis/clinical-table/

2. Fontana E, Dansette PM, Poli SM. (2005) Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. Curr. Drug Metab., 6 (5): 413-54. [PMID:16248836]

3. Furster C, Wikvall K. (1999) Identification of CYP3A4 as the major enzyme responsible for 25-hydroxylation of 5beta-cholestane-3alpha,7alpha,12alpha-triol in human liver microsomes. Biochim. Biophys. Acta, 1437 (1): 46-52. [PMID:9931427]

4. Kharasch ED, Mitchell D, Coles R, Blanco R. (2008) Rapid clinical induction of hepatic cytochrome P4502B6 activity by ritonavir. Antimicrob. Agents Chemother., 52 (5): 1663-9. [PMID:18285471]

5. Shahrokh K, Cheatham 3rd TE, Yost GS. (2012) Conformational dynamics of CYP3A4 demonstrate the important role of Arg212 coupled with the opening of ingress, egress and solvent channels to dehydrogenation of 4-hydroxy-tamoxifen. Biochim. Biophys. Acta, 1820 (10): 1605-17. [PMID:22677141]

How to cite this family page

Database page citation:

CYP3 family. Accessed on 12/07/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=263.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Enzymes. Br J Pharmacol. 172: 6024-6109.