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 synthase), a potential target for the treatment of hormone dependent and hormone independent malignancies

2007/09/18 by Michael C. Byrns, Stephan Steckelbroeck, Trevor M. Penning +1 · 30 citations
Biochemistry, Genetics and Molecular Biology · Medicine · #Aldose Reductase and Taurine #Prenatal Substance Exposure Effects #Eicosanoids and Hypertension Pharmacology

paper · doi:10.1016/j.bcp.2007.09.008

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• AKR1C Isoforms Represent a Novel Cellular Target for Jasmonates alongside Their Mitochondrial-Mediated Effects
• Conversion of Classical and 11-Oxygenated Androgens by Insulin-Induced AKR1C3 in a Model of Human PCOS Adipocytes
• Aldo-Keto Reductases and Cancer Drug Resistance
• AKR1C3 as a potential target for the inhibitory effect of dietary flavonoids
• Reduction of secondary 3-keto bile acids by aldo-keto reductase 1C1 and 1C4
• Intracrine androgen metabolism in prostate cancer progression: mechanisms of castration resistance and therapeutic implications. [europepmc]
• The aldo-keto reductase superfamily and its role in drug metabolism and detoxification. [europepmc]
• Type 5 17beta-hydroxysteroid dehydrogenase/prostaglandin F synthase (AKR1C3): role in breast cancer and inhibition by non-steroidal anti-inflammatory drug analogs. [europepmc]
• Steroid hormone transforming aldo-keto reductases and cancer. [europepmc]
• Lack of functional and expression homology between human and mouse aldo-keto reductase 1C enzymes: implications for modelling human cancers. [europepmc]
• Aldo-keto reductase 1C3 expression in MCF-7 cells reveals roles in steroid hormone and prostaglandin metabolism that may explain its over-expression in breast cancer. [europepmc]
• Partners in crime: deregulation of AR activity and androgen synthesis in prostate cancer. [europepmc]
• New frontiers in androgen biosynthesis and metabolism. [europepmc]
• Inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3): overview and structural insights. [europepmc]
• Substrate specificity and inhibitor analyses of human steroid 5β-reductase (AKR1D1). [europepmc]
• Intratumoral de novo steroid synthesis activates androgen receptor in castration-resistant prostate cancer and is upregulated by treatment with CYP17A1 inhibitors. [europepmc]
• Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships. [europepmc]
• Overexpression of aldo-keto reductase 1C3 (AKR1C3) in LNCaP cells diverts androgen metabolism towards testosterone resulting in resistance to the 5α-reductase inhibitor finasteride. [europepmc]
• Distinct patterns of dysregulated expression of enzymes involved in androgen synthesis and metabolism in metastatic prostate cancer tumors. [europepmc]
• Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer. [europepmc]
• AKR1C3 as a target in castrate resistant prostate cancer. [europepmc]
• Role of aldo-keto reductase family 1 (AKR1) enzymes in human steroid metabolism. [europepmc]
• The aldo-keto reductases (AKRs): Overview. [europepmc]
• Mechanisms of drug resistance that target the androgen axis in castration resistant prostate cancer (CRPC). [europepmc]
• Aldo-Keto Reductase AKR1C1-AKR1C4: Functions, Regulation, and Intervention for Anti-cancer Therapy. [europepmc]
• Aldo-Keto Reductase (AKR) 1C3 inhibitors: a patent review. [europepmc]
• AKR1C enzymes sustain therapy resistance in paediatric T-ALL. [europepmc]
• AKR1C3 (type 5 17β-hydroxysteroid dehydrogenase/prostaglandin F synthase): Roles in malignancy and endocrine disorders. [europepmc]
• Structural and Functional Biology of Aldo-Keto Reductase Steroid-Transforming Enzymes. [europepmc]
• Potent and Highly Selective Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors Act as Chemotherapeutic Potentiators in Acute Myeloid Leukemia and T-Cell Acute Lymphoblastic Leukemia. [europepmc]