1.-.-.- Oxidoreductases

Home
Targets
Enzymes
1.-.-.- Oxidoreductases

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

3222

aldehyde dehydrogenase 2 family member Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2595

Nomenclature

aldehyde dehydrogenase 2 family member

Previous and unofficial names

aldehyde dehydrogenase 2, mitochondrial | aldehyde dehydrogenase 2 family (mitochondrial) | aldehyde dehydrogenase 2

Genes

ALDH2 (Hs), Aldh2 (Mm), Aldh2 (Rn)

Ensembl ID

ENSG00000111275 (Hs), ENSMUSG00000029455 (Mm), ENSRNOG00000037815 (Rn)

UniProtKB AC

P05091 (Hs), P47738 (Mm), P11884 (Rn)

EC number

1.2.1.3

an aldehyde + H₂O + NAD = a carboxylate + 2H⁺ + NADH

Inhibitors

prunetin pK_i 6.3 (In vitro inhibition of recombinant human mitochondrial alcohol dehydrogenase) [9]

aldo-keto reductase family 1 member B Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2768

Nomenclature

aldo-keto reductase family 1 member B

Previous and unofficial names

Genes

AKR1B1 (Hs), Akr1b1 (Mm), Akr1b1 (Rn)

Ensembl ID

ENSG00000085662 (Hs), ENSMUSG00000001642 (Mm), ENSRNOG00000009513 (Rn)

UniProtKB AC

P15121 (Hs), P45376 (Mm), P07943 (Rn)

EC number

1.1.1.21

Inhibitors

tolrestat pIC₅₀ 7.3 [15]

VAP-1 (amine oxidase copper containing 3) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2767

Nomenclature

amine oxidase copper containing 3

Common abbreviation

VAP-1

Previous and unofficial names

Genes

AOC3 (Hs), Aoc3 (Mm), Aoc3 (Rn)

Ensembl ID

ENSG00000131471 (Hs), ENSMUSG00000019326 (Mm), ENSRNOG00000051307 (Rn)

UniProtKB AC

Q16853 (Hs), O70423 (Mm), O08590 (Rn)

EC number

1.4.3.21

Inhibitors

phenelzine pIC₅₀ 7.7 [11]

Selective inhibitors

PXS-4728A pIC₅₀ 8.3 [14]

Antibodies

timolumab (Binding) pK_d 9.4 – 9.9 [16]

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

Target Id

2979

Nomenclature

catalase

Previous and unofficial names

Cas1 | Cas-1

Genes

CAT (Hs), Cat (Mm), Cat (Rn)

Ensembl ID

ENSG00000121691 (Hs), ENSMUSG00000027187 (Mm), ENSRNOG00000008364 (Rn)

UniProtKB AC

P04040 (Hs), P24270 (Mm), P04762 (Rn)

EC number

1.11.1.6
Conversion of the reactive oxygen species hydrogen peroxide to water and oxygen. 2 H₂O₂ <=> O₂ + 2 H₂O

Activators

tectorigenin [21] - Hamster

Comment

Catalase is a heme-containing enzyme that protects cells from the damaging effects of the reactive oxygen species hydrogen peroxide (H₂O₂).

DHFR (dihydrofolate reductase) C Show summary »« Hide summary More detailed page go icon to follow link

DHODH (dihydroorotate dehydrogenase (quinone)) C Show summary »« Hide summary More detailed page go icon to follow link

glutathione-disulfide reductase Show summary »« Hide summary More detailed page go icon to follow link

hydroxy-delta-5-steroid dehydrogenase, 3 beta- and steroid delta-isomerase 2 Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2622

Nomenclature

hydroxy-delta-5-steroid dehydrogenase, 3 beta- and steroid delta-isomerase 2

Previous and unofficial names

3 beta-hydroxysteroid dehydrogenase/Delta 5 | Hsd3b2 | hydroxy-delta-5-steroid dehydrogenase, 3 beta- and steroid delta-isomerase 1 | hydroxy-delta-5-steroid dehydrogenase

Genes

HSD3B2 (Hs), Hsd3b1 (Mm), Hsd3b1 (Rn)

Ensembl ID

ENSG00000203859 (Hs), ENSMUSG00000027871 (Mm), ENSRNOG00000070622 (Rn)

UniProtKB AC

P26439 (Hs), P24815 (Mm)

EC number

1.1.1.145

5.3.3.1

Inhibitors

trilostane pIC₅₀ 8.4 (Note that the species is not specified in the referenced article.) [12]

4-hydroxyphenylpyruvate dioxygenase Show summary »« Hide summary More detailed page go icon to follow link

11-βHSD1 (hydroxysteroid 11-beta dehydrogenase 1) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2763

Nomenclature

hydroxysteroid 11-beta dehydrogenase 1

Common abbreviation

11-βHSD1

Previous and unofficial names

11β-HSD | 11b-HSD | corticosteroid 11-beta-dehydrogenase isozyme 1 | HSD11B | hydroxysteroid (11-beta) dehydrogenase 1

Genes

HSD11B1 (Hs), Hsd11b1 (Mm), Hsd11b1 (Rn)

Ensembl ID

ENSG00000117594 (Hs), ENSMUSG00000016194 (Mm), ENSRNOG00000005861 (Rn)

UniProtKB AC

P28845 (Hs), P50172 (Mm), P16232 (Rn)

EC number

1.1.1.146

11-βHSD2 (hydroxysteroid 11-beta dehydrogenase 2) Show summary »« Hide summary More detailed page go icon to follow link

hydroxysteroid 17-beta dehydrogenase 2 Show summary »« Hide summary More detailed page go icon to follow link

Target Id

3094

Nomenclature

hydroxysteroid 17-beta dehydrogenase 2

Previous and unofficial names

17β-HSD2 | estradiol 17-beta-dehydrogenase 2 | HSD17 | SDR9C2 | short chain dehydrogenase/reductase family 9C, member 2

Genes

HSD17B2 (Hs), Hsd17b2 (Mm), Hsd17b2 (Rn)

Ensembl ID

ENSG00000086696 (Hs), ENSMUSG00000031844 (Mm), ENSRNOG00000013982 (Rn)

UniProtKB AC

P37059 (Hs), P51658 (Mm)

EC number

1.1.1.62

17β-estradiol + NAD⁺ = estrone + H⁺ + NADH

1.1.1.239

Comment

17β-HSD2 catalyses the interconversion of estradiol <-> estrone and testosterone <-> androstenedione.

hydroxysteroid 17-beta dehydrogenase 13 Show summary »« Hide summary

Target Id

3222

Nomenclature

hydroxysteroid 17-beta dehydrogenase 13

Genes

HSD17B13 (Hs), Hsd17b13 (Mm), Hsd17b13 (Rn)

Ensembl ID

ENSG00000170509 (Hs), ENSMUSG00000034528 (Mm), ENSRNOG00000002212 (Rn)

UniProtKB AC

Q7Z5P4 (Hs), Q8VCR2 (Mm), Q5M875 (Rn)

Inhibitors

BI-3231 [18]

Comment

HSD17B13 is a novel drug target for nonalcoholic steatohepatitis (NASH) and other liver diseases. Estradiol and leukotriene B₄ (LTB₄) are potential HSD17B13 substrates [18].

IMPDH1 (inosine monophosphate dehydrogenase 1) C Show summary »« Hide summary More detailed page go icon to follow link

IMPDH2 (inosine monophosphate dehydrogenase 2) C Show summary »« Hide summary More detailed page go icon to follow link

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

Target Id	2789
Nomenclature	myeloperoxidase
Genes	MPO (Hs), Mpo (Mm), Mpo (Rn)
Ensembl ID	ENSG00000005381 (Hs), ENSMUSG00000009350 (Mm), ENSRNOG00000008310 (Rn)
UniProtKB AC	P05164 (Hs), P11247 (Mm)
Comment	Myeloperoxidase is a therapeutic target for the development of novel treatments for inflammation-related cardiovascular diseases.

sepiapterin reductase Show summary »« Hide summary More detailed page go icon to follow link

Target Id

3020

Nomenclature

sepiapterin reductase

Previous and unofficial names

SDR38C1 | sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming) | short chain dehydrogenase/reductase family 38C, member 1

Genes

SPR (Hs), Spr (Mm), Spr (Rn)

Ensembl ID

ENSG00000116096 (Hs), ENSMUSG00000033735 (Mm), ENSRNOG00000015455 (Rn)

UniProtKB AC

P35270 (Hs), P18297 (Rn)

EC number

1.1.1.153
De novo synthesis of tetrahydrobiopterin from GTP, and synthesis of the erythro form of tetrahydrobiopterin L-erythro-7,8-dihydrobiopterin + NADP(+) <=> sepiapterin + NADPH L-erythro-tetrahydrobiopterin + 2 NADP(+) <=> 6-pyruvoyl-5,6,7,8-tetrahydropterin + 2 NADPH

steroid 5 alpha-reductase 2 Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2633

Nomenclature

steroid 5 alpha-reductase 2

Previous and unofficial names

3-oxo-5-alpha-steroid 4-dehydrogenase 2 | steroid-5-alpha-reductase, alpha polypeptide 2 (3-oxo-5 alpha-steroid delta 4-dehydrogenase alpha 2)

Genes

SRD5A2 (Hs), Srd5a2 (Mm), Srd5a2 (Rn)

Ensembl ID

ENSG00000277893 (Hs), ENSMUSG00000038541 (Mm), ENSRNOG00000027042 (Rn)

UniProtKB AC

P31213 (Hs), Q99N99 (Mm), P31214 (Rn)

EC number

1.3.99.5

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

Target Id

2643

Nomenclature

tyrosinase

Previous and unofficial names

OCA1A | OCAIA

Genes

TYR (Hs), Tyr (Mm), Tyr (Rn)

Ensembl ID

ENSG00000077498 (Hs), ENSMUSG00000004651 (Mm), ENSRNOG00000016421 (Rn)

UniProtKB AC

P14679 (Hs), P11344 (Mm)

EC number

1.14.18.1

Inhibitors

compound 7 [PMID: 21334791] pIC₅₀ 6.4 [17]

Comment

Because tyrosinase is essential for the biosynthesis of melanin it has been proposed as a molecular target for the treatment of skin hyperpigmentation. Tyrosinase can oxidize dopamine to generate melanin in the brain, a process that is implicated in the pathogenesis of Parkinson's disease neurodegeneration [1].

vitamin K epoxide reductase complex subunit 1 Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2645

Nomenclature

vitamin K epoxide reductase complex subunit 1

Previous and unofficial names

vitamin K epoxide reductase complex, subunit 1 | vitamin K epoxide reductase complex

Genes

VKORC1 (Hs), Vkorc1 (Mm), Vkorc1 (Rn)

Ensembl ID

ENSG00000167397 (Hs), ENSMUSG00000096145 (Mm), ENSRNOG00000050828 (Rn)

UniProtKB AC

Q9BQB6 (Hs), Q9CRC0 (Mm), Q6TEK4 (Rn)

EC number

1.1.4.1

Inhibitors

alitretinoin [7,20]

dicumarol [6]

phenindione [4,19]

phenprocoumon [4]

Selective inhibitors

warfarin pK_i 5.6 [2]

Comment

Subunit of the vitamin K epoxide reductase enzyme. The exact structure of the complex is not specified in the available literature.

XDH (xanthine dehydrogenase) C Show summary »« Hide summary More detailed page go icon to follow link

References

Show »« Hide

1. Asanuma M, Miyazaki I, Ogawa N. (2003) Dopamine- or L-DOPA-induced neurotoxicity: the role of dopamine quinone formation and tyrosinase in a model of Parkinson's disease. Neurotox Res, 5 (3): 165-76. [PMID:12835121]

2. Bevans CG, Krettler C, Reinhart C, Tran H, Koßmann K, Watzka M, Oldenburg J. (2013) Determination of the warfarin inhibition constant Ki for vitamin K 2,3-epoxide reductase complex subunit-1 (VKORC1) using an in vitro DTT-driven assay. Biochim Biophys Acta, 1830 (8): 4202-10. [PMID:23618698]

3. Evenäs J, Edfeldt F, Lepistö M, Svitacheva N, Synnergren A, Lundquist B, Gränse M, Rönnholm A, Varga M, Wright J et al.. (2014) HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase. Bioorg Med Chem Lett, 24 (5): 1315-21. [PMID:24508129]

4. FIELD JB, GOLDFARB MS, WARE AG, GRIFFITH GC. (1952) Effect in man of a new indandione anticoagulant. Proc Soc Exp Biol Med, 81 (3): 678-81. [PMID:13037763]

5. Heikkilä T, Ramsey C, Davies M, Galtier C, Stead AM, Johnson AP, Fishwick CW, Boa AN, McConkey GA. (2007) Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase. J Med Chem, 50 (2): 186-91. [PMID:17228860]

6. Hollman A. (1991) Dicoumarol and warfarin. Br Heart J, 66 (2): 181. [PMID:18610395]

7. Keller C, Matzdorff AC, Kemkes-Matthes B. (1999) Pharmacology of warfarin and clinical implications. Semin Thromb Hemost, 25 (1): 13-6. [PMID:10327215]

8. Liu X, Sturla SJ. (2009) Profiling patterns of glutathione reductase inhibition by the natural product illudin S and its acylfulvene analogues. Mol Biosyst, 5 (9): 1013-24. [PMID:19668867]

9. Lowe ED, Gao GY, Johnson LN, Keung WM. (2008) Structure of daidzin, a naturally occurring anti-alcohol-addiction agent, in complex with human mitochondrial aldehyde dehydrogenase. J Med Chem, 51 (15): 4482-7. [PMID:18613661]

10. Nelson PH, Eugui E, Wang CC, Allison AC. (1990) Synthesis and immunosuppressive activity of some side-chain variants of mycophenolic acid. J Med Chem, 33 (2): 833-8. [PMID:1967654]

11. Nurminen EM, Pihlavisto M, Lázár L, Szakonyi Z, Pentikäinen U, Fülöp F, Pentikäinen OT. (2010) Synthesis, in vitro activity, and three-dimensional quantitative structure-activity relationship of novel hydrazine inhibitors of human vascular adhesion protein-1. J Med Chem, 53 (17): 6301-15. [PMID:20690686]

12. Rabe T, Kiesel L, Kellermann J, Weidenhammer K, Runnebaum B, Potts GO. (1983) Inhibition of human placental progesterone synthesis and aromatase activity by synthetic steroidogenic inhibitors in vitro. Fertil Steril, 39 (6): 829-35. [PMID:6574022]

13. Rosowsky A, Mota CE, Queener SF, Waltham M, Ercikan-Abali E, Bertino JR. (1995) 2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii. J Med Chem, 38 (5): 745-52. [PMID:7877140]

14. Schilter HC, Collison A, Russo RC, Foot JS, Yow TT, Vieira AT, Tavares LD, Mattes J, Teixeira MM, Jarolimek W. (2015) Effects of an anti-inflammatory VAP-1/SSAO inhibitor, PXS-4728A, on pulmonary neutrophil migration. Respir Res, 16: 42. [PMID:25889951]

15. Singh SB, Malamas MS, Hohman TC, Nilakantan R, Carper DA, Kitchen D. (2000) Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants. J Med Chem, 43 (6): 1062-70. [PMID:10737739]

16. Smith DJ, Vainio P, Mikkola J, Vuorio P, Vainio J. (2011) Fully human anti-VAP-1 monoclonal antibodies. Patent number: US7897149 B2. Assignee: Biotie Therapies Corp.. Priority date: 20/04/2007. Publication date: 01/03/2011.

17. Tajima R, Oozeki H, Muraoka S, Tanaka S, Motegi Y, Nihei H, Yamada Y, Masuoka N, Nihei K. (2011) Synthesis and evaluation of bibenzyl glycosides as potent tyrosinase inhibitors. Eur J Med Chem, 46 (4): 1374-81. [PMID:21334791]

18. Thamm S, Willwacher MK, Aspnes GE, Bretschneider T, Brown NF, Buschbom-Helmke S, Fox T, Gargano EM, Grabowski D, Hoenke C et al.. (2023) Discovery of a Novel Potent and Selective HSD17B13 Inhibitor, BI-3231, a Well-Characterized Chemical Probe Available for Open Science. J Med Chem, 66 (4): 2832-2850. [PMID:36727857]

19. TOOHEY M. (1952) Antagonism of anticoagulants dicoumarol, tromexan, and phenylindandione by vitamin K. Br Med J, 2 (4786): 687-90. [PMID:12978288]

20. Wallin R, Wajih N, Hutson SM. (2008) VKORC1: a warfarin-sensitive enzyme in vitamin K metabolism and biosynthesis of vitamin K-dependent blood coagulation factors. Vitam Horm, 78: 227-46. [PMID:18374197]

21. Zhang R, Piao MJ, Oh MC, Park JE, Shilnikova K, Moon YJ, Kim DH, Jung U, Kim IG, Hyun JW. (2016) Protective Effect of an Isoflavone, Tectorigenin, Against Oxidative Stress-induced Cell Death via Catalase Activation. J Cancer Prev, 21 (4): 257-263. [PMID:28053960]

How to cite this family page

Database page citation:

1.-.-.- Oxidoreductases. Accessed on 11/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=840.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.