C. Supuran

Challenges and opportunities in the drug design and pharmacological applications of MMP inhibitors.

Overview of matrix metalloproteinases (MMPs) in health and disease.

Multitargeted Anticancer Activities: Cathepsin B–Carbonic Anhydrase IX/XII Inhibitors Show Enhanced Cytotoxicity Against Lung Adenocarcinoma Cells

The multi‐target inhibition of two significant cancer drug targets, cathepsin B and human carbonic anhydrase (hCA) isoforms IX and XII has been explored. The exclusive synthesis of single isomeric structure of final compounds despite two possibilities, in vitro biological studies, in silico molecular docking, DFT and A...

From Identification to Enzymatic Activity Profiling: Comprehensive Characterization of BloCAβ, a Probiotic β‐Carbonic Anhydrase From Bifidobacterium longum

The first biochemical and functional characterization of β‐class carbonic anhydrase from Bifidobacterium longum (BloCAβ) by inhibition and activation profiles is reported, establishing a biochemical basis for future studies investigating the physiological role of probiotic CAs in bacterial models.

Harnessing coumarin privilege to achieve potency and selectivity: hypoxia-targeted alkyl coumarin-tethered phenyl quinazolinones as dual hCA IX/HSP90α inhibitors with chemosensitizing activity

A series of alkyl coumarin-tethered phenyl quinazolinones were rationally designed and synthesized as hypoxia-targeted dual hCA IX/HSP90α inhibitors, exhibiting potent, highly selective inhibition of hCA IX (in the nanomolar range), while displaying negligible activity against the off-target isoforms hCA I and II.

Synthesis and Biological Evaluation of Indole‐Benzene Sulfonamides as Carbonic Anhydrase II, IX, and XII Inhibitors

Human carbonic anhydrases (hCAs) are zinc‐bound enzymes that play a critical role in pH regulation and ion balance. Among them, isoforms hCA IX and XII are overexpressed in tumor hypoxia and are implicated in tumor progression. In this study, new indole‐benzenesulfonamide derivatives with hydrazide and amide linkers we...