Paragi G

ORCID: 0000-0001-5408-1748 · 2 papers in corpus

2026

Targeting Steroid-Metabolizing Enzymes with 15β-Substituted Estrone Analogues: Dual Discovery of AKR1C2/17β-HSD1 Inhibitors and a Fluorescent 17β-HSD1 Ligand

Cancers ·doi:10.3390/cancers18121889

Background/objectivesAldo-keto reductase isoforms AKR1C1-3 and 17β-hydroxysteroid dehydrogenase 1 and 2 (17β-HSD1 and 17β-HSD2) are key enzymes in steroid metabolism and validated targets in hormone-dependent cancers.MethodsIn this study, Δ…

2021

Synthesis and evaluation of AKR1C inhibitory properties of A-ring halogenated oestrone derivatives.

Journal of enzyme inhibition and medicinal chemistry ·doi:10.1080/14756366.2021.1937142

Enzymes AKR1C regulate the action of oestrogens, androgens, and progesterone at the pre-receptor level and are also associated with chemo-resistance. The activities of these oestrone halides were investigated on recombinant AKR1C enzymes. T…