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 …
(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 …
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 …
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 …
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
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 …
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 …
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 …
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) …
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 …
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 …
groups in a number of important steroid and prostanoid molecules. The enzyme is also over …