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 …
Isatin and its derivatives: a survey of recent syntheses, reactions, and applications
R Kakkar - MedChemComm, 2019 - pubs.rsc.org
Isatin (1H-indole-2, 3-dione) and its derivatives represent an important class of heterocyclic
compounds that can be used as precursors for drug synthesis. Since its discovery, a lot of …
compounds that can be used as precursors for drug synthesis. Since its discovery, a lot of …
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 …
Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors
Abstract Carbonic anhydrase (CA, EC 4.2. 1.1) is an enzyme and a very omnipresent zinc
metalloenzyme which catalyzed the reversible hydration and dehydration of carbon dioxide …
metalloenzyme which catalyzed the reversible hydration and dehydration of carbon dioxide …
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 …
Advances in the structural annotation of human carbonic anhydrases and impact on future drug discovery
A Nocentini, CT Supuran - Expert Opinion on Drug Discovery, 2019 - Taylor & Francis
Introduction: Of the 15 human carbonic anhydrase (CA, EC 4.2. 1.1) isoforms known to date,
for 11 the crystal structure is known. Many different classes of CA inhibitors (CAIs) were …
for 11 the crystal structure is known. Many different classes of CA inhibitors (CAIs) were …
A decade of tail-approach based design of selective as well as potent tumor associated carbonic anhydrase inhibitors
Human carbonic anhydrase (hCA) isoforms hCA IX and hCA XII are well established
anticancer drug targets and their selective inhibition is highly desired for the proper …
anticancer drug targets and their selective inhibition is highly desired for the proper …
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 …
Exploring the multiple binding modes of inhibitors to carbonic anhydrases for novel drug discovery
CT Supuran - Expert opinion on drug discovery, 2020 - Taylor & Francis
Introduction The spacious active site cavity of the metalloenzyme carbonic anhydrase (CA,
EC 4.2. 1.1) shows a great versatility for a variety of binding modes for modulators of activity …
EC 4.2. 1.1) shows a great versatility for a variety of binding modes for modulators of activity …
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) …