CYP1 family | Enzymes | IUPHAR/BPS Guide to PHARMACOLOGY

CYP1 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).

Overview

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CYP1 enzymes catalyse the generation of highly mutagenic compounds via activation of procarcinogens (such as polycyclic aromatic hydrocarbons and aromatic amines) that are present in combustion products. They can also deactivate many anticancer agents [4].

Enzymes

CYP1A1 C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1318

Nomenclature

CYP1A1

Previous and unofficial names

Genes

CYP1A1 (Hs), Cyp1a1 (Mm), Cyp1a1 (Rn)

Ensembl ID

ENSG00000140465 (Hs), ENSMUSG00000032315 (Mm), ENSRNOG00000019500 (Rn)

UniProtKB AC

P04798 (Hs), P00184 (Mm), P00185 (Rn)

EC number

1.14.1.1

Inhibitors

65PF pIC₅₀ 6.8 [3]

Comment

CYP1A1 is an extra-hepatic enzyme. It shows a preference for linear planar aromatic molecules [5].

CYP1A2 C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1319

Nomenclature

CYP1A2

Previous and unofficial names

cytochrome P450, subfamily I (aromatic compound-inducible), polypeptide 2 | cytochrome P450 1A2 | Cytochrome P450 subfamily I (aromatic compound-inducible) member A2 (Q42 form d) | cytochrome P450, family 1, subfamily A, polypeptide 2 | cytochrome P450 | cytochrome P450, family 1, subfamily a, polypeptide 2

Genes

CYP1A2 (Hs), Cyp1a2 (Mm), Cyp1a2 (Rn)

Ensembl ID

ENSG00000140505 (Hs), ENSMUSG00000032310 (Mm), ENSRNOG00000016173 (Rn)

UniProtKB AC

P05177 (Hs), P00186 (Mm), P04799 (Rn)

EC number

1.14.1.1

Inhibitors

5H78PF pIC₅₀ 7.8 [3]

Comment

CYP1A2 is constitutively expressed in liver. It shows a preference for triangular planar aromatic molecules [5].

CYP1B1 C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1320

Nomenclature

CYP1B1

Previous and unofficial names

GLC3A | cytochrome P450, subfamily I (dioxin-inducible), polypeptide 1 (glaucoma 3, primary infantile) | cytochrome P450, subfamily 1B, polypeptide 1 | cytochrome P450, family 1, subfamily B, polypeptide 1 | cytochrome P450, family 1, subfamily b, polypeptide 1 | cytochrome P450

Genes

CYP1B1 (Hs), Cyp1b1 (Mm), Cyp1b1 (Rn)

Ensembl ID

ENSG00000138061 (Hs), ENSMUSG00000024087 (Mm), ENSRNOG00000040287 (Rn)

UniProtKB AC

Q16678 (Hs), Q64429 (Mm), Q64678 (Rn)

EC number

1.14.1.1

Inhibitors

stilbenes [2]

Comment

Mainly expressed in extra-hepatic tissues such as breast, prostate and uterus. Can metabolise 17β-estradiol into a mutagen [2], as well as leukotrienes and eicosanoids [1]. Gene variants have been associated with primary congenitial glaucoma [6].

Comments

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References

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1. Divanovic S, Dalli J, Jorge-Nebert LF, Flick LM, Gálvez-Peralta M, Boespflug ND, Stankiewicz TE, Fitzgerald JM, Somarathna M, Karp CL et al.. (2013) Contributions of the three CYP1 monooxygenases to pro-inflammatory and inflammation-resolution lipid mediator pathways. J Immunol, 191 (6): 3347-57. [PMID:23956430]

2. Dutour R, Poirier D. (2017) Inhibitors of cytochrome P450 (CYP) 1B1. Eur J Med Chem, 135: 296-306. [PMID:28458135]

3. Liu J, Taylor SF, Dupart PS, Arnold CL, Sridhar J, Jiang Q, Wang Y, Skripnikova EV, Zhao M, Foroozesh M. (2013) Pyranoflavones: a group of small-molecule probes for exploring the active site cavities of cytochrome P450 enzymes 1A1, 1A2, and 1B1. J Med Chem, 56 (10): 4082-92. [PMID:23600958]

4. McFadyen MC, McLeod HL, Jackson FC, Melvin WT, Doehmer J, Murray GI. (2001) Cytochrome P450 CYP1B1 protein expression: a novel mechanism of anticancer drug resistance. Biochem Pharmacol, 62 (2): 207-12. [PMID:11389879]

5. Sridhar J, Goyal N, Liu J, Foroozesh M. (2017) Review of Ligand Specificity Factors for CYP1A Subfamily Enzymes from Molecular Modeling Studies Reported to-Date. Molecules, 22 (7). [PMID:28698457]

6. Vasiliou V, Gonzalez FJ. (2008) Role of CYP1B1 in glaucoma. Annu Rev Pharmacol Toxicol, 48: 333-58. [PMID:17914928]

How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2019) The Concise Guide to PHARMACOLOGY 2019/20: Enzymes. Br J Pharmacol. 176 Issue S1: S297-S396.