CYP5, CYP7 and CYP8 families | Enzymes | IUPHAR/BPS Guide to PHARMACOLOGY

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Cytochrome P450
CYP5, CYP7 and CYP8 families

CYP5, CYP7 and CYP8 families 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).

Enzymes

Thromboxane synthase (CYP5A1) C Show summary »« Hide summary More detailed page

Target Id

1353

Nomenclature

CYP5A1

Common abbreviation

Thromboxane synthase

Previous and unofficial names

Genes

TBXAS1 (Hs), Tbxas1 (Mm), Tbxas1 (Rn)

Ensembl ID

ENSG00000059377 (Hs), ENSMUSG00000029925 (Mm), ENSRNOG00000007918 (Rn)

UniProtKB AC

P24557 (Hs), P36423 (Mm), P49430 (Rn)

EC number

5.3.99.5

PGH₂ = thromboxane A₂

Inhibitors

ozagrel pIC₅₀ 8.4 [6]

Comment

Inhibited by dazoxiben [9], camonagrel [4] and furegrelate sodium (U-63557A: PubChem CID 23663954) [2].

Prostacyclin synthase (CYP8A1) C Show summary »« Hide summary

CYP7A1 C Show summary »« Hide summary

Target Id

1354

Nomenclature

CYP7A1

Previous and unofficial names

Genes

CYP7A1 (Hs), Cyp7a1 (Mm), Cyp7a1 (Rn)

Ensembl ID

ENSG00000167910 (Hs), ENSMUSG00000028240 (Mm), ENSRNOG00000009488 (Rn)

UniProtKB AC

P22680 (Hs), Q64505 (Mm), P18125 (Rn)

EC number

1.14.14.23

Comment

Converts cholesterol to 7α-hydroxycholesterol [8].

CYP7B1 C Show summary »« Hide summary

Target Id

1355

Nomenclature

CYP7B1

Previous and unofficial names

Genes

CYP7B1 (Hs), Cyp7b1 (Mm), Cyp7b1 (Rn)

Ensembl ID

ENSG00000172817 (Hs), ENSMUSG00000039519 (Mm), ENSRNOG00000009730 (Rn)

UniProtKB AC

O75881 (Hs), Q60991 (Mm), Q63688 (Rn)

EC number

1.14.14.29

Comment

Converts dehydroepiandrosterone to 7α-DHEA [10].

CYP8B1 C Show summary »« Hide summary

Target Id

1357

Nomenclature

CYP8B1

Previous and unofficial names

Genes

CYP8B1 (Hs), Cyp8b1 (Mm), Cyp8b1 (Rn)

Ensembl ID

ENSG00000180432 (Hs), ENSMUSG00000050445 (Mm), ENSRNOG00000019481 (Rn)

UniProtKB AC

Q9UNU6 (Hs), O88962 (Mm)

EC number

1.14.14.139

1.14.18.8

Comment

Converts 7α-hydroxycholest-4-en-3-one to 7-alpha,12α-dihydroxycholest-4-en-3-one (in rabbit) [7] in the biosynthesis of bile acids.

References

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1. Faull AW, Brewster AG, Brown GR, Smithers MJ, Jackson R. (1995) Dual-acting thromboxane receptor antagonist/synthase inhibitors: synthesis and biological properties of [2-substituted-4-(3-pyridyl)-1,3-dioxan-5-yl] alkenoic acids. J. Med. Chem., 38 (4): 686-94. [PMID:7861416]

2. Gorman RR, Johnson RA, Spilman CH, Aiken JW. (1983) Inhibition of platelet thromboxane A2 synthase activity by sodium 5-(3'-pyridinylmethyl)benzofuran-2-carboxylate. Prostaglandins, 26 (2): 325-42. [PMID:6316421]

3. Gryglewski RJ, Bunting S, Moncada S, Flower RJ, Vane JR. (1976) Arterial walls are protected against deposition of platelet thrombi by a substance (prostaglandin X) which they make from prostaglandin endoperoxides. Prostaglandins, 12 (5): 685-713. [PMID:824685]

4. Gryglewski RJ, Szczeklik A, Korbut R, Swies J, Musiał J, Krzanowski M, Maga P. (1995) The mechanism of anti-thrombotic, thrombolytic and fibrinolytic actions of camonagrel--a new thromboxane synthase inhibitor. Wien. Klin. Wochenschr., 107 (9): 283-9. [PMID:7778318]

5. Hatae T, Hara S, Yokoyama C, Yabuki T, Inoue H, Ullrich V, Tanabe T. (1996) Site-directed mutagenesis of human prostacyclin synthase: Alteration of Cys441 of the Cys-pocket, and Glu347 and Arg350 of the EXXR motif. FEBS Lett., 389 (3): 268-72. [PMID:8766713]

6. Hiraku S, Taniguchi K, Wakitani K, Omawari N, Kira H, Miyamoto T, Okegawa T, Kawasaki A, Ujiie A. (1986) Pharmacological studies on the TXA2 synthetase inhibitor (E)-3-[p-(1H-imidazol-1-ylmethyl)phenyl]-2-propenoic acid (OKY-046). Jpn. J. Pharmacol., 41 (3): 393-401. [PMID:3093741]

7. Ishida H, Noshiro M, Okuda K, Coon MJ. (1992) Purification and characterization of 7 alpha-hydroxy-4-cholesten-3-one 12 alpha-hydroxylase. J. Biol. Chem., 267 (30): 21319-23. [PMID:1400444]

8. Noshiro M, Okuda K. (1990) Molecular cloning and sequence analysis of cDNA encoding human cholesterol 7 alpha-hydroxylase. FEBS Lett., 268 (1): 137-40. [PMID:2384150]

9. Randall MJ, Parry MJ, Hawkeswood E, Cross PE, Dickinson RP. (1981) UK-37, 248, a novel, selective thromboxane synthetase inhibitor with platelet anti-aggregatory and anti-thrombotic activity. Thromb. Res., 23 (1-2): 145-62. [PMID:6795753]

10. Rose KA, Stapleton G, Dott K, Kieny MP, Best R, Schwarz M, Russell DW, Björkhem I, Seckl J, Lathe R. (1997) Cyp7b, a novel brain cytochrome P450, catalyzes the synthesis of neurosteroids 7alpha-hydroxy dehydroepiandrosterone and 7alpha-hydroxy pregnenolone. Proc. Natl. Acad. Sci. U.S.A., 94 (10): 4925-30. [PMID:9144166]

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.