Multiple binding modes of inhibitors to carbonic anhydrases: how to design specific drugs targeting 15 different isoforms?

V Alterio, A Di Fiore, K D'Ambrosio, CT Supuran… - Chemical …, 2012 - ACS Publications
Carbonic anhydrases (CAs, EC 4.2. 1.1) are ubiquitous metallo-enzymes, present
throughout most living organisms and encoded by five evolutionarily unrelated gene …

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 anhydrases: novel therapeutic applications for inhibitors and activators

CT Supuran - Nature reviews Drug discovery, 2008 - nature.com
Carbonic anhydrases (CAs), a group of ubiquitously expressed metalloenzymes, are
involved in numerous physiological and pathological processes, including …

Carbonic anhydrase inhibitors

CT Supuran - Bioorganic & medicinal chemistry letters, 2010 - Elsevier
Carbonic anhydrases (CAs, EC 4.2. 1.1) are widespread enzymes in all organisms,
catalyzing CO2 hydration to bicarbonate and protons. Their inhibition is exploited clinically …

Carbonic anhydrase as a model for biophysical and physical-organic studies of proteins and protein− ligand binding

VM Krishnamurthy, GK Kaufman, AR Urbach… - Chemical …, 2008 - ACS Publications
Carbonic anhydrase (CA, EC 4.2. 1.1) is a protein that is especially well-suited to serve as a
model in many types of studies in biophysics, bioanalysis, the physical-organic chemistry of …

Carbonic anhydrases as targets for medicinal chemistry

CT Supuran, A Scozzafava - Bioorganic & medicinal chemistry, 2007 - Elsevier
Carbonic anhydrases (CAs, EC 4.2. 1.1) are zinc enzymes acting as efficient catalysts for the
reversible hydration of carbon dioxide to bicarbonate. 16 different α-CA isoforms were …

Non-zinc mediated inhibition of carbonic anhydrases: coumarins are a new class of suicide inhibitors

A Maresca, C Temperini, H Vu, NB Pham… - Journal of the …, 2009 - ACS Publications
The X-ray crystal structure of the adduct between the zinc metalloenzyme carbonic
anhydrase II (CA, EC 4.2. 1.1) with the recently discovered natural product coumarin …

Carbonic anhydrases-an overview

CT Supuran - Current pharmaceutical design, 2008 - ingentaconnect.com
Carbonic anhydrases (CAs, EC 4.2. 1.1) are widespread metalloenzymes all over the
phylogenetic tree, with at least 4 distinct gene families encoding for them. At least 16 …

Deciphering the mechanism of carbonic anhydrase inhibition with coumarins and thiocoumarins

A Maresca, C Temperini, L Pochet… - Journal of medicinal …, 2010 - ACS Publications
Coumarin derivatives were recently shown to constitute a totally new class of inhibitors of the
zinc metalloenzyme carbonic anhydrase (CA, EC 4.2. 1.1), being hydrolyzed within the CA …

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 …