Carbonic anhydrase inhibitors as emerging agents for the treatment and imaging of hypoxic tumors

CT Supuran - Expert opinion on investigational drugs, 2018 - Taylor & Francis
Introduction: Hypoxic tumors overexpress two carbonic anhydrases (CA, EC 4.2. 1.1), CA IX
and XII, involved in complex processes connected to tumorigenesis (pH regulation …

Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: three for the price of one

CT Supuran, V Alterio, A Di Fiore… - Medicinal Research …, 2018 - Wiley Online Library
Human carbonic anhydrase (CA) IX is a tumor‐associated protein, since it is scarcely
present in normal tissues, but highly overexpressed in a large number of solid tumors, where …

Carbonic anhydrase inhibition and the management of hypoxic tumors

CT Supuran - Metabolites, 2017 - mdpi.com
Hypoxia and acidosis are salient features of many tumors, leading to a completely different
metabolism compared to normal cells. Two of the simplest metabolic products, protons and …

Aromatic sulfonamides including a sulfonic acid tail: new membrane impermeant carbonic anhydrase inhibitors for targeting selectively the cancer-associated isoforms

S Giovannuzzi, M D'Ambrosio, C Luceri… - International Journal of …, 2021 - mdpi.com
We report here a new drug design strategy for producing membrane-impermeant carbonic
anhydrase (CA; EC 4.2. 1.1) inhibitors selectively targeting the tumor-associated, membrane …

Azidothymidine “Clicked” into 1, 2, 3-triazoles: first report on carbonic anhydrase–telomerase dual-hybrid inhibitors

E Berrino, A Angeli, DD Zhdanov… - Journal of medicinal …, 2020 - ACS Publications
Cancer cells rely on the enzyme telomerase (EC 2.7. 7.49) to promote cellular immortality.
Telomerase inhibitors (ie, azidothymidine) can represent promising antitumor agents …

α-CAs from photosynthetic organisms

E Langella, A Di Fiore, V Alterio, SM Monti… - International Journal of …, 2022 - mdpi.com
Carbonic anhydrases (CAs) are ubiquitous enzymes that catalyze the reversible carbon
dioxide hydration reaction. Among the eight different CA classes existing in nature, the α …

Novel approaches for designing drugs that interfere with pH regulation

E Berrino, CT Supuran - Expert Opinion on Drug Discovery, 2019 - Taylor & Francis
Introduction: In all living species, pH regulation is a tightly controlled process, with a plethora
of proteins involved in its regulation. These include sodium-proton exchangers, carbonic …

[HTML][HTML] Carbonic anhydrase IX subcellular localization in normoxic and hypoxic SH-SY5Y neuroblastoma cells is assisted by its C-terminal protein interaction domain

M Succoio, S Amiranda, E Sasso, C Marciano, A Finizio… - Heliyon, 2023 - cell.com
The human carbonic anhydrase IX (CA IX) is a hypoxia-induced transmembrane protein
belonging to the α-CA enzyme family. It has a crucial role in pH regulation in hypoxic cells …

Post-translational modifications in tumor-associated carbonic anhydrases

A Di Fiore, CT Supuran, A Scaloni, G De Simone - Amino Acids, 2022 - Springer
Human carbonic anhydrases IX (hCA IX) and XII (hCA XII) are two proteins associated with
tumor formation and development. These enzymes have been largely investigated both from …

Intrinsically disordered features of carbonic anhydrase IX proteoglycan-like domain

E Langella, M Buonanno, G De Simone… - Cellular and Molecular …, 2021 - Springer
Abstract hCA IX is a multi-domain protein belonging to the family of hCAs which are
ubiquitous zinc enzymes that catalyze the reversible hydration of CO 2 to HCO 3− and H+ …