Emerging role of carbonic anhydrase inhibitors
CT Supuran - Clinical Science, 2021 - portlandpress.com
Inhibition of carbonic anhydrase (CA, EC 4.2. 1.1) was clinically exploited for decades, as
most modern diuretics were obtained considering as lead molecule acetazolamide, the …
most modern diuretics were obtained considering as lead molecule acetazolamide, the …
A simple yet multifaceted 90 years old, evergreen enzyme: Carbonic anhydrase, its inhibition and activation
CT Supuran - Bioorganic & Medicinal Chemistry Letters, 2023 - Elsevier
Advances in the carbonic anhydrase (CA, EC 4.2. 1.1) research over the last three decades
are presented, with an emphasis on the deciphering of the activation mechanism, the …
are presented, with an emphasis on the deciphering of the activation mechanism, the …
Incorporating selenium into heterocycles and natural products─ from chemical properties to pharmacological activities
W Hou, H Xu - Journal of Medicinal Chemistry, 2022 - ACS Publications
Selenium (Se)-containing compounds have emerged as potential therapeutic agents for the
treatment of a range of diseases. Through tremendous effort, considerable knowledge has …
treatment of a range of diseases. Through tremendous effort, considerable knowledge has …
Carbonic anhydrase inhibitors targeting metabolism and tumor microenvironment
The tumor microenvironment is crucial for the growth of cancer cells, triggering particular
biochemical and physiological changes, which frequently influence the outcome of …
biochemical and physiological changes, which frequently influence the outcome of …
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 …
present in normal tissues, but highly overexpressed in a large number of solid tumors, where …
Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase
Inorganic anions inhibit the metalloenzyme carbonic anhydrase (CA, EC 4.2. 1.1) generally
by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA …
by coordinating to the active site metal ion. Cyanate was reported as a non-coordinating CA …
Experimental carbonic anhydrase inhibitors for the treatment of hypoxic tumors
CT Supuran - Journal of Experimental Pharmacology, 2020 - Taylor & Francis
Abstract Carbonic anhydrase (CA, EC 4.2. 1.1) isoforms IX and XII are overexpressed in
many hypoxic tumors as a consequence of the hypoxia inducible factor (HIF) activation …
many hypoxic tumors as a consequence of the hypoxia inducible factor (HIF) activation …
1, 5-diaryl-1, 2, 4-triazole ureas as new SLC-0111 analogues endowed with dual carbonic anhydrase and VEGFR-2 inhibitory activities
Presently, dual targeting by a single small molecule stands out as an effective cancer-
fighting weapon. Carbonic anhydrase (CA) and vascular-endothelial growth factor (VEGF) …
fighting weapon. Carbonic anhydrase (CA) and vascular-endothelial growth factor (VEGF) …
Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII
In this work, different series of benzothiazole-based sulphonamides 8a-c, 10, 12, 16a-b and
carboxylic acids 14a-c were developed as novel SLC-0111 analogues with the goal of …
carboxylic acids 14a-c were developed as novel SLC-0111 analogues with the goal of …
Multiple Binding Modes of Inhibitors to Human Carbonic Anhydrases: An Update on the Design of Isoform-Specific Modulators of Activity
K D'Ambrosio, A Di Fiore, V Alterio, E Langella… - Chemical …, 2024 - ACS Publications
Human carbonic anhydrases (hCAs) are widespread zinc enzymes that catalyze the
hydration of CO2 to bicarbonate and a proton. Currently, 15 isoforms have been identified, of …
hydration of CO2 to bicarbonate and a proton. Currently, 15 isoforms have been identified, of …