AKR1C3 as a target in castrate resistant prostate cancer
Open accessAbstract
Aberrant androgen receptor (AR) activation is the major driver of castrate resistant prostate cancer (CRPC). CRPC is ultimately fatal and more therapeutic agents are needed to treat this disease. Compounds that target the androgen axis by inhibiting androgen biosynthesis and or AR signaling are potential candidates for use in CRPC treatment and are currently being pursued aggressively. Aldo-keto reductase 1C3 (AKR1C3) plays a pivotal role in androgen biosynthesis within the prostate. It catalyzes the 17-ketoreduction of weak androgen precursors to give testosterone and 5α-dihydrotestosterone. AKR1C3 expression and activity has been implicated in the development of CRPC, making it a rational target. Selective inhibition of AKR1C3 will be important, however, due to the presence of closely related isoforms, AKR1C1 and AKR1C2 that are also involved in androgen inactivation. We examine the evidence that supports the vital role of AKR1C3 in CRPC and recent developments in the discovery of potent and selective AKR1C3 inhibitors. This article is part of a Special Issue entitled 'CSR 2013'.
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AKR1C3 is overexpressed in prostate cancer, presumably promoting cancer progression by increasing intratumoral androgen levels.
“AKR1C3 is also overexpressed in prostate cancer, presumably promoting cancer progression by increasing intratumoral androgen levels (Adeniji et al., 2013, Fung et al., 2006).”
From Intracrine androgen biosynthesis, metabolism and action revisited (2018) · cites this paper as Adeniji et al., 2013
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Self-citation
- Authors
- Adeniji, A. O., Chen, M., & Penning, T. M.
- Affiliations
- University of Pennsylvania (US)
- Corresponding author
- Penning, Trevor M.
- Venue
- The Journal of Steroid Biochemistry and Molecular Biology
- Publisher
- Elsevier BV
- Published
- 2013-09
- Volume
- 137
- Pages
- 136-149
- ISSN
- 0960-0760 (ISSN-L)
- PMC
- PMC3805777
- OpenAlex
- W2075145938
- Cited by
- 143
- References
- 82
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- FWCI
- 2.49
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- The Journal of Steroid Biochemistry and Molecular Biology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- Prostate Cancer Foundation Challenge Grant
- TAPITMAT
- Topics
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Prostate Cancer Treatment and Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Aldose Reductase and Taurine
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
- Keywords
- AKR1C3, castration-resistant prostate cancer, androgen production, androgen receptor, AKR1C1, AKR1C2, AKR1C3 inhibitors, dihydrotestosterone, testosterone
- MeSH terms
- Aldo-Keto Reductase Family 1 Member C3, Humans, Hydroxyprostaglandin Dehydrogenases, Male, Orchiectomy, Prostatic Neoplasms, 3-Hydroxysteroid Dehydrogenases
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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