Top ▲

AKR1C3

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 1382

Nomenclature: AKR1C3

Family: Prostaglandin synthases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 323 10p15.1 AKR1C3 aldo-keto reductase family 1 member C3
Mouse - 323 13 A1 Akr1c18 aldo-keto reductase family 1, member C18
Rat - 323 17q12.2 Akr1c3 aldo-keto reductase family 1, member C3
Previous and Unofficial Names Click here for help
Aldo-keto reductase family 1 member C3 | prostaglandin F synthase | 17β-HSD 5 | 17β-hydroxysteroid dehydrogenase type 5 | 3α-hydroxysteroid dehydrogenase type 2 | dihydrodiol dehydrogenase 3 | dihydrodiol dehydrogenase type I | PGFS | hydroxysteroid (17-beta) dehydrogenase 5 | 20 alpha-hydroxysteroid dehydrogenase | 20-alpha-HSD | Akr1c18 | aldo-keto reductase family 1 member C18 | HSD1 | aldo-keto reductase family 1, member C3 | aldo-keto reductase family 1
Database Links Click here for help
Alphafold P42330 (Hs), Q8K023 (Mm), P51652 (Rn)
BRENDA 1.1.1.188, 1.3.1.20, 1.1.1.213, 1.1.1.239, 1.1.1.64
CATH/Gene3D 3.20.20.100
ChEMBL Target CHEMBL4681 (Hs)
Ensembl Gene ENSG00000196139 (Hs), ENSMUSG00000021214 (Mm), ENSRNOG00000017531 (Rn)
Entrez Gene 8644 (Hs), 105349 (Mm), 171516 (Rn)
Human Protein Atlas ENSG00000196139 (Hs)
KEGG Enzyme 1.1.1.188, 1.3.1.20, 1.1.1.213, 1.1.1.239, 1.1.1.64
KEGG Gene hsa:8644 (Hs), mmu:105349 (Mm), rno:171516 (Rn)
OMIM 603966 (Hs)
Pharos P42330 (Hs)
UniProtKB P42330 (Hs), Q8K023 (Mm), P51652 (Rn)
Wikipedia AKR1C3 (Hs)
Enzyme Reaction Click here for help
EC Number: 1.1.1.188 PGD2 + NADP+ = PGF2α + NADPH + H+
EC Number: 1.3.1.20
EC Number: 1.1.1.213
EC Number: 1.1.1.239
EC Number: 1.1.1.64
Inhibitors (Human)
flufenamic acid, indomethacin, flavonoids such as 2'-hydroxyflavanone (pIC50 6.5)  [2,4]

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
tolfenamic acid Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition 8.1 pKi 3
⤷ pKi 8.1 (Ki 8x10-9 M) [3]
compound 1 [Lolli et al., 2019] Small molecule or natural product Primary target of this compound Hs Inhibition 6.5 pIC50 1
⤷ pIC50 6.5 (IC50 3x10-7 M) [1]
KV-37 Small molecule or natural product Hs Inhibition - - 5
⤷ [5]

References

Show »

1. Lolli ML, Carnovale IM, Pippione AC, Wahlgren WY, Bonanni D, Marini E, Zonari D, Gallicchio M, Boscaro V, Goyal P et al.. (2019) Bioisosteres of Indomethacin as Inhibitors of Aldo-Keto Reductase 1C3. ACS Med Chem Lett, 10 (4): 437-443. DOI: 10.1021/acsmedchemlett.8b00484 [PMID:30996776]

2. Matsuura K, Shiraishi H, Hara A, Sato K, Deyashiki Y, Ninomiya M, Sakai S. (1998) Identification of a principal mRNA species for human 3alpha-hydroxysteroid dehydrogenase isoform (AKR1C3) that exhibits high prostaglandin D2 11-ketoreductase activity. J Biochem, 124 (5): 940-6. [PMID:9792917]

3. Qiu W, Zhou M, Mazumdar M, Azzi A, Ghanmi D, Luu-The V, Labrie F, Lin SX. (2007) Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase. J Biol Chem, 282 (11): 8368-79. [PMID:17166832]

4. Skarydová L, Zivná L, Xiong G, Maser E, Wsól V. (2009) AKR1C3 as a potential target for the inhibitory effect of dietary flavonoids. Chem Biol Interact, 178 (1-3): 138-44. [PMID:19007764]

5. Verma K, Gupta N, Zang T, Wangtrakluldee P, Srivastava SK, Penning TM, Trippier PC. (2018) AKR1C3 Inhibitor KV-37 Exhibits Antineoplastic Effects and Potentiates Enzalutamide in Combination Therapy in Prostate Adenocarcinoma Cells. Mol Cancer Ther, 17 (9): 1833-1845. [PMID:29891491]

Contributors

Show »

How to cite this page