CYP24, CYP26 and CYP27 families | Enzymes | IUPHAR/BPS Guide to PHARMACOLOGY

CYP24, CYP26 and CYP27 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).

GtoImmuPdb view: OFF

Enzymes

CYP24A1 C Show summary »« Hide summary

Target Id

1365

Nomenclature

CYP24A1

Previous and unofficial names

Genes

CYP24A1 (Hs), Cyp24a1 (Mm), Cyp24a1 (Rn)

Ensembl ID

ENSG00000019186 (Hs), ENSMUSG00000038567 (Mm), ENSRNOG00000013062 (Rn)

UniProtKB AC

Q07973 (Hs), Q64441 (Mm), Q09128 (Rn)

EC number

1.14.13.126

Inhibitors

compound 3a [PMID: 15615534] pIC₅₀ 8.1 [3]

MK-24 pIC₅₀ 8.1 [3]

compound 4d [PMID: 20655626] pIC₅₀ 4.8 [1]

Comment

Converts 1,25-dihydroxyvitamin D3 (calcitriol) to 1α,24R,25-trihydroxyvitamin D₃.

CYP26A1 C Show summary »« Hide summary More detailed page

Target Id

1366

Nomenclature

CYP26A1

Previous and unofficial names

Genes

CYP26A1 (Hs), Cyp26a1 (Mm), Cyp26a1 (Rn)

Ensembl ID

ENSG00000095596 (Hs), ENSMUSG00000024987 (Mm), ENSRNOG00000016750 (Rn)

UniProtKB AC

O43174 (Hs), O55127 (Mm)

EC number

1.14.-.-

Selective inhibitors

compound 5 [PMID: 21838328] pIC₅₀ 9.5 [2]

Comment

Converts retinoic acid to 4-hydroxyretinoic acid. Inhibited by liarozole

CYP26B1 C Show summary »« Hide summary

Target Id

1367

Nomenclature

CYP26B1

Previous and unofficial names

Retinoic acid-metabolizing cytochrome | cytochrome P450 26B1 | cytochrome P450 | cytochrome P450, family 26, subfamily B, polypeptide 1

Genes

CYP26B1 (Hs), Cyp26b1 (Mm), Cyp26b1 (Rn)

Ensembl ID

ENSG00000003137 (Hs), ENSMUSG00000063415 (Mm), ENSRNOG00000015076 (Rn)

UniProtKB AC

Q9NR63 (Hs), Q811W2 (Mm), G3V7X8 (Rn)

EC number

1.14.-.-

Comment

Converts retinoic acid to 4-hydroxyretinoic acid.

CYP26C1 Show summary »« Hide summary

Sterol 27-hydroxylase (CYP27A1) C Show summary »« Hide summary

Target Id

1369

Nomenclature

CYP27A1

Common abbreviation

Sterol 27-hydroxylase

Previous and unofficial names

Genes

CYP27A1 (Hs), Cyp27a1 (Mm), Cyp27a1 (Rn)

Ensembl ID

ENSG00000135929 (Hs), ENSMUSG00000026170 (Mm), ENSRNOG00000017188 (Rn)

UniProtKB AC

Q02318 (Hs), Q9DBG1 (Mm), P17178 (Rn)

EC number

1.14.13.15

Inhibitors

compound 4d [PMID: 20655626] pIC₅₀ 7.2 [1]

MK-24 pIC₅₀ <6.0 [3]

Comment

Converts cholesterol to 27-hydroxycholesterol.

CYP27B1 C Show summary »« Hide summary

Target Id

1370

Nomenclature

CYP27B1

Previous and unofficial names

calcidiol 1-monooxygenase | VD3 1A hydroxylase | cytochrome P450 40 (25-hydroxyvitamin D3 1 alpha-hydroxylase) | cytochrome P450, family 27, subfamily B, polypeptide 1 | cytochrome P450

Genes

CYP27B1 (Hs), Cyp27b1 (Mm), Cyp27b1 (Rn)

Ensembl ID

ENSG00000111012 (Hs), ENSMUSG00000006724 (Mm), ENSRNOG00000046214 (Rn)

UniProtKB AC

O15528 (Hs), O35084 (Mm), O35132 (Rn)

EC number

1.14.13.13

Inhibitors

MK-24 pIC₅₀ 6.3 [3]

Comment

Converts 25-hydroxyvitamin D₃ to 1,25-dihydroxyvitamin D3 (calcitriol)

CYP27C1 Show summary »« Hide summary

Target Id

1371

Nomenclature

CYP27C1

Previous and unofficial names

cytochrome P450, family 27, subfamily C, polypeptide 1

Genes

CYP27C1 (Hs)

Ensembl ID

ENSG00000186684 (Hs)

UniProtKB AC

Q4G0S4 (Hs)

EC number

1.14.-.-

References

Show »« Hide

1. Aboraia AS, Makowski B, Bahja A, Prosser D, Brancale A, Jones G, Simons C. (2010) Synthesis and CYP24A1 inhibitory activity of (E)-2-(2-substituted benzylidene)- and 2-(2-substituted benzyl)-6-methoxy-tetralones. Eur J Med Chem, 45 (10): 4427-34. [PMID:20655626]

2. Gomaa MS, Bridgens CE, Veal GJ, Redfern CP, Brancale A, Armstrong JL, Simons C. (2011) Synthesis and biological evaluation of 3-(1H-imidazol- and triazol-1-yl)-2,2-dimethyl-3-[4-(naphthalen-2-ylamino)phenyl]propyl derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26). J. Med. Chem., 54 (19): 6803-11. [PMID:21838328]

3. Kahraman M, Sinishtaj S, Dolan PM, Kensler TW, Peleg S, Saha U, Chuang SS, Bernstein G, Korczak B, Posner GH. (2004) Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3). J. Med. Chem., 47 (27): 6854-63. [PMID:15615534]

How to cite this family page

Database page citation:

CYP24, CYP26 and CYP27 families. Accessed on 12/07/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=267.

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.