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GeneE
28 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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AKR1C3
aldo-keto reductase family 1 member C3
Chromosome 10 · 10p15.1
NCBI Gene: 8644Ensembl: ENSG00000196139.14HGNC: HGNC:386UniProt: A0A0A0MSS8
210PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Hub Gene
RESEARCH IMPACT
Trending
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionretinal dehydrogenase (NAD+) activitycellular response to calcium ioncellular response to prostaglandin stimulusprostate cancerhepatocellular carcinomaFamilial prostate cancerposterior cortical atrophy
✦AI Summary

AKR1C3 is a cytosolic aldo-keto reductase that catalyzes NADPH-dependent reduction of ketosteroids to hydroxysteroids with broad substrate specificity 12. In androgen metabolism, AKR1C3 converts Δ4-androstenedione to testosterone in the classical pathway and reduces androsterone to 5α-androstane-3α,17β-diol in the alternative 'backdoor' pathway, both producing potent androgens 13. It also reduces estrone to 17β-estradiol and functions as a prostaglandin F2α synthase 12. Mechanistically, NADPH's abundance drives net reductase activity in vivo despite bidirectional in vitro potential 24. Clinically, AKR1C3 is significantly upregulated in multiple cancers with poor prognostic implications. In hepatocellular carcinoma, AKR1C3-dependent lipid droplet formation confers sorafenib resistance by regulating lipid and energy homeostasis 5, while an AKR1C3/NF-κB/STAT3 positive feedback loop drives proliferation and metastasis 6. In esophageal adenocarcinoma, AKR1C3 enhances radioresistance by inhibiting ferroptosis through HSPA5 stabilization 7. In castrate-resistant prostate cancer, AKR1C3-mediated testosterone production from weak androgen precursors maintains AR signaling 8, with dual AKR1C3/AR-variant inhibitors showing synergy with standard therapies 9. AKR1C3 inhibitors (indomethacin, medroxyprogesterone acetate) demonstrate therapeutic potential across these malignancies 610.

Sources cited
1
In hepatocellular carcinoma, AKR1C3-dependent lipid droplet formation confers sorafenib resistance by regulating lipid and energy homeostasis , while an AKR1C3/NF-κB/STAT3 positive feedback loop drives proliferation and metastasis .
PMID: 36451864
2
In hepatocellular carcinoma, AKR1C3-dependent lipid droplet formation confers sorafenib resistance by regulating lipid and energy homeostasis , while an AKR1C3/NF-κB/STAT3 positive feedback loop drives proliferation and metastasis .
PMID: 33361392
3
In esophageal adenocarcinoma, AKR1C3 enhances radioresistance by inhibiting ferroptosis through HSPA5 stabilization .
PMID: 40603306
4
In castrate-resistant prostate cancer, AKR1C3-mediated testosterone production from weak androgen precursors maintains AR signaling , with dual AKR1C3/AR-variant inhibitors showing synergy with standard therapies .
PMID: 23748150
5
In castrate-resistant prostate cancer, AKR1C3-mediated testosterone production from weak androgen precursors maintains AR signaling , with dual AKR1C3/AR-variant inhibitors showing synergy with standard therapies .
PMID: 39088701
Disease Associationsⓘ20
prostate cancerOpen Targets
0.12Weak
hepatocellular carcinomaOpen Targets
0.11Weak
Familial prostate cancerOpen Targets
0.11Weak
posterior cortical atrophyOpen Targets
0.10Weak
esophageal adenocarcinomaOpen Targets
0.09Suggestive
gastric cancerOpen Targets
0.09Suggestive
neoplasmOpen Targets
0.09Suggestive
primary ovarian insufficiencyOpen Targets
0.08Suggestive
small cell lung carcinomaOpen Targets
0.08Suggestive
46,XX gonadal dysgenesisOpen Targets
0.07Suggestive
liver cancerOpen Targets
0.07Suggestive
polycystic ovary syndromeOpen Targets
0.07Suggestive
premature ovarian failure 19Open Targets
0.07Suggestive
premature ovarian failure 1Open Targets
0.06Suggestive
invasive hydatidiform moleOpen Targets
0.06Suggestive
premature ovarian failure 22Open Targets
0.06Suggestive
oocyte/zygote/embryo maturation arrest 17Open Targets
0.06Suggestive
oocyte/zygote/embryo maturation arrest 20Open Targets
0.06Suggestive
Familial hyperprolactinemiaOpen Targets
0.06Suggestive
familial hyperprolactinemiaOpen Targets
0.06Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
CYP1B1Protein interaction98%CYP3A5Protein interaction98%CYP11B1Protein interaction98%CYP11B2Protein interaction98%CYP17A1Protein interaction98%CYP19A1Protein interaction98%
Tissue Expression6 tissues
Liver
100%
Bone Marrow
20%
Lung
19%
Heart
11%
Ovary
6%
Brain
3%
Gene Interaction Network
Click a node to explore
AKR1C3CYP1B1CYP3A5CYP11B1CYP11B2CYP17A1CYP19A1
PROTEIN STRUCTURE
Preparing viewer…
PDB1S1P · 1.20 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.34LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.99 [0.74–1.34]
RankingsWhere AKR1C3 stands among ~20K protein-coding genes
  • #1,984of 20,598
    Most Researched210 · top 10%
  • #14,026of 17,882
    Most Constrained (LOEUF)1.34
Genes detectedAKR1C3
Sources retrieved28 papers
Response time—
📄 Sources
28▼
1
AKR1C3-dependent lipid droplet formation confers hepatocellular carcinoma cell adaptability to targeted therapy.
PMID: 36451864
Theranostics · 2022
1.00
2
Identification and functional validation of ACSL1 as a biomarker regulating ferroptosis in nucleus pulposus cell.
PMID: 40042449
Biosci Rep · 2025
0.92
3
A Positive Feedback Loop of AKR1C3-Mediated Activation of NF-κB and STAT3 Facilitates Proliferation and Metastasis in Hepatocellular Carcinoma.
PMID: 33361392
Cancer Res · 2021
0.90
4
Inhibition of the glucocorticoid-activating enzyme 11β-hydroxysteroid dehydrogenase type 1 drives concurrent 11-oxygenated androgen excess.
PMID: 38551804
FASEB J · 2024
0.84
5
Overview of AKR1C3: Inhibitor Achievements and Disease Insights.
PMID: 32463235
J Med Chem · 2020
0.80