Inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3): overview and structural insights

MC Byrns, Y Jin, TM Penning - The Journal of steroid biochemistry and …, 2011 - Elsevier
There is considerable interest in the development of an inhibitor of aldo–keto reductase
(AKR) 1C3 (type 5 17β-hydroxysteroid dehydrogenase and prostaglandin F synthase) as a …

Overview of AKR1C3: inhibitor achievements and disease insights

Y Liu, S He, Y Chen, Y Liu, F Feng, W Liu… - Journal of medicinal …, 2020 - ACS Publications
Human aldo-keto reductase family 1 member C3 (AKR1C3) is known as a hormone activity
regulator and prostaglandin F (PGF) synthase that regulates the occupancy of hormone …

Development of novel AKR1C3 inhibitors as new potential treatment for castration-resistant prostate cancer

S Endo, H Oguri, J Segawa, M Kawai… - Journal of medicinal …, 2020 - ACS Publications
Aldo–keto reductase (AKR) 1C3 catalyzes the synthesis of active androgens that promote
the progression of prostate cancer. AKR1C3 also contributes to androgen-independent cell …

Androgen synthesis in adrenarche

WL Miller - Reviews in Endocrine and Metabolic Disorders, 2009 - Springer
The enzymes and pathways of steroidogenesis are central to an understanding of
adrenarche. The quantitative regulation of steroidogenesis occurs at the first step, the …

Design and validation of specific inhibitors of 17β-hydroxysteroid dehydrogenases for therapeutic application in breast and prostate cancer, and in endometriosis

JM Day, HJ Tutill, A Purohit… - Endocrine-related …, 2008 - erc.bioscientifica.com
Advanced medullary thyroid cancers (MTCs) are now being treated with drugs that inhibit
receptor tyrosine kinases, many of which involved in angiogenesis. Response rates vary …

An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3α-HSD, type 5 17β-HSD, and prostaglandin F …

MC Byrns, S Steckelbroeck, TM Penning - Biochemical pharmacology, 2008 - Elsevier
Aldo-keto reductase (AKR) 1C3 (type 2 3α-HSD, type 5 17β-HSD, and prostaglandin F
synthase) regulates ligand access to steroid hormone and prostaglandin receptors and may …

Spirolactones: Recent advances in natural products, bioactive compounds and synthetic strategies

A Quintavalla - Current Medicinal Chemistry, 2018 - ingentaconnect.com
Background: The spirocyclic compounds have always aroused a great interest because this
motif is present as structural core in a number of natural products and bioactive compounds …

Binary and ternary crystal structure analyses of a novel inhibitor with 17β-HSD type 1: a lead compound for breast cancer therapy

M Mazumdar, D Fournier, DW Zhu, C Cadot… - Biochemical …, 2009 - portlandpress.com
Oestradiol is a well-characterized sex hormone that stimulates breast cancer and other
oestrogen-related diseases. 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) …

Ruthenium complexes show potent inhibition of AKR1C1, AKR1C2, and AKR1C3 enzymes and anti-proliferative action against chemoresistant ovarian cancer cell …

J Kljun, R Pavlič, E Hafner, T Lipec… - Frontiers in …, 2022 - frontiersin.org
In this study, we present the synthesis, kinetic studies of inhibitory activity toward aldo-keto
reductase 1C (AKR1C) enzymes, and anticancer potential toward chemoresistant ovarian …

Crystal structures of three classes of non-steroidal anti-inflammatory drugs in complex with aldo-keto reductase 1C3

JU Flanagan, Y Yosaatmadja, RM Teague, MZL Chai… - 2012 - journals.plos.org
Aldo-keto reductase 1C3 (AKR1C3) catalyses the NADPH dependent reduction of carbonyl
groups in a number of important steroid and prostanoid molecules. The enzyme is also over …