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 …

How many carbonic anhydrase inhibition mechanisms exist?

CT Supuran - Journal of enzyme inhibition and medicinal chemistry, 2016 - Taylor & Francis
Six genetic families of the enzyme carbonic anhydrase (CA, EC 4.2. 1.1) were described to
date. Inhibition of CAs has pharmacologic applications in the field of antiglaucoma …

Advances in structure-based drug discovery of carbonic anhydrase inhibitors

CT Supuran - Expert opinion on drug discovery, 2017 - Taylor & Francis
Introduction: The enzyme carbonic anhydrase (CA, EC 4.2. 1.1) is found in numerous
organisms across the tree of life, with seven distinct classes known to date. CA inhibition can …

Carbonic anhydrase inhibitors targeting metabolism and tumor microenvironment

A Angeli, F Carta, A Nocentini, JY Winum… - Metabolites, 2020 - mdpi.com
The tumor microenvironment is crucial for the growth of cancer cells, triggering particular
biochemical and physiological changes, which frequently influence the outcome of …

Rational approaches, design strategies, structure activity relationship and mechanistic insights for anticancer hybrids

K Nepali, S Sharma, M Sharma, PMS Bedi… - European journal of …, 2014 - Elsevier
A Hybrid drug which comprises the incorporation of two drug pharmacophores in one single
molecule are basically designed to interact with multiple targets or to amplify its effect …

Structure-based drug discovery of carbonic anhydrase inhibitors

CT Supuran - Journal of enzyme inhibition and medicinal chemistry, 2012 - Taylor & Francis
Inhibition of the metalloenzyme carbonic anhydrase (CA; EC 4.2. 1.1) has pharmacologic
applications in the field of anti-glaucoma, anti-convulsant and anti-cancer agents. But …

Discovery of a new family of carbonic anhydrases in the malaria pathogen Plasmodium falciparum—The η-carbonic anhydrases

S Del Prete, D Vullo, GM Fisher, KT Andrews… - Bioorganic & Medicinal …, 2014 - Elsevier
The genome of the protozoan parasite Plasmodium falciparum, the causative agent of the
most lethal type of human malaria, contains a single gene annotated as encoding a carbonic …

Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase

A Nocentini, A Angeli, F Carta, JY Winum… - Journal of Enzyme …, 2021 - Taylor & Francis
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 …

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 …

Design, synthesis, and biological activity of novel dithiocarbamate‐methylsulfonyl hybrids as carbonic anhydrase inhibitors

D Osmaniye, C Türkeş, Y Demir, Y Özkay… - Archiv der …, 2022 - Wiley Online Library
Carbonic anhydrase (CA) enzymes are involved in many physiological events. These
enzymes, which contain Zn2+ in their structure, can be easily inhibited by dithiocarbamate …