AKR1C3 | Prostaglandin synthases | IUPHAR/BPS Guide to PHARMACOLOGY

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AKR1C3

Target not currently curated in GtoImmuPdb

Target id: 1382

Nomenclature: AKR1C3

Family: Prostaglandin synthases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - AKR1C3 aldo-keto reductase family 1 member C3
Mouse - - Akr1c18 aldo-keto reductase family 1, member C18
Rat - - Akr1c3 aldo-keto reductase family 1
Previous and Unofficial Names
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
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 1.1.1.188 PGD2 + NADP+ = PGF + 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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
tolfenamic acid Hs Inhibition 8.1 pKi 3
pKi 8.1 (Ki 8x10-9 M) [3]
compound 1 [Lolli et al., 2019] Hs Inhibition 6.5 pIC50 1
pIC50 6.5 (IC50 3x10-7 M) [1]
KV-37 Hs Inhibition - - 5
[5]

References

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1. Lolli ML, Carnovale IM, Pippione AC, Wahlgren WY, Bananni 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 Medicinal Chemistry Letters, Article ASAP. DOI: 10.1021/acsmedchemlett.8b00484

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

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How to cite this page

Angelo A. Izzo.
Prostaglandin synthases: AKR1C3. Last modified on 21/03/2019. Accessed on 16/06/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1382.