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Special Issue Editor

Prof. Dr. Maria Novella Romanelli

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Department of Neuroscience, Psychology, Drug Research and Child’s Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
Interests: enzyme modulators; ion channel modulators; multi-target ligands; antihyperalgesic agents; receptor modulators
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Special Issue Information

Dear Colleagues,

Carbonic anhydrase (CA, EC 4.2.1.1.) is a widespread enzyme that catalyzes the reversible hydration of CO₂ to HCO₃ and H⁺. This simple reaction has a pivotal role in many physiological processes, and its deregulation is involved in different pathological states. For a long time, CA inhibitors have been used as diuretics and to treat conditions such as altitude sickness, obesity, some forms of epilepsy, and glaucoma. In recent times, other possible medical applications have been discovered, such as anticancer, pain-relieving, and anti-infective. Indeed, suitable drug targets are not only mammal isoforms but also the isozymes present in pathogens (bacteria, fungi and protozoa). In addition, considerable interest has emerged for CA activators since genetic deficiencies of some human isoforms have been linked to the outbreak of different pathologic conditions.

This Special Issue aims to collect research papers and short communication, as well as short focused reviews, to provide an overview of recent advances in the design, synthesis, and biological evaluation of CA modulators for the many biomedical applications involving these enzymes.

Prof. Dr. Maria Novella Romanelli
Guest Editor

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Keywords

Drug design
Chemical synthesis
Biological activity
Molecular modeling
X-ray crystallography
Drug targets
Carbonic anhydrase inhibitors
Carbonic anhydrase activators
Neurodegenerative diseases
Cancer
Pain
Epilepsy
Infectious diseases
Polypharmacology

Published Papers (2 papers)

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Research

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15 pages, 5193 KiB

Open AccessArticle

New Histamine-Related Five-Membered N-Heterocycle Derivatives as Carbonic Anhydrase I Activators

by Niccolò Chiaramonte, Alessio Gabellini, Andrea Angeli, Gianluca Bartolucci, Laura Braconi, Silvia Dei, Elisabetta Teodori, Claudiu T. Supuran and Maria Novella Romanelli

Molecules 2022, 27(2), 545; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27020545 - 15 Jan 2022

Cited by 2 | Viewed by 2108

Abstract

A series of histamine (HST)-related compounds were synthesized and tested for their activating properties on five physiologically relevant human Carbonic Anhydrase (hCA) isoforms (I, II, Va, VII and XIII). The imidazole ring of HST was replaced with different 5-membered heterocycles and the length of the aliphatic chain was varied. For the most interesting compounds some modifications on the terminal amino group were also performed. The most sensitive isoform to activation was hCA I (K_A values in the low micromolar range), but surprisingly none of the new compounds displayed activity on hCA II. Some derivatives (1, 3a and 22) displayed an interesting selectivity for activating hCA I over hCA II, Va, VII and XIII. Full article

(This article belongs to the Special Issue Carbonic Anhydrases-Chemistry and Biomedical Applications)

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Review

Jump to: Research

36 pages, 18640 KiB

Open AccessReview

Carbonic Anhydrase Activators for Neurodegeneration: An Overview

by Valeria Poggetti, Silvia Salerno, Emma Baglini, Elisabetta Barresi, Federico Da Settimo and Sabrina Taliani

Molecules 2022, 27(8), 2544; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27082544 - 14 Apr 2022

Cited by 16 | Viewed by 2922

Abstract

Carbonic anhydrases (CAs) are a family of ubiquitous metal enzymes catalyzing the reversible conversion of CO₂ and H₂O to HCO₃⁻ with the release of a proton. They play an important role in pH regulation and in the balance of body fluids and are involved in several functions such as homeostasis regulation and cellular respiration. For these reasons, they have been studied as targets for the development of agents for treating several pathologies. CA inhibitors have been used in therapy for a long time, especially as diuretics and for the treatment of glaucoma, and are being investigated for application in other pathologies including obesity, cancer, and epilepsy. On the contrary, CAs activators are still poorly studied. They are proposed to act as additional (other than histidine) proton shuttles in the rate-limiting step of the CA catalytic cycle, which is the generation of the active hydroxylated enzyme. Recent studies highlight the involvement of CAs activation in brain processes essential for the transmission of neuronal signals, suggesting CAs activation might represent a potential therapeutic approach for the treatment of Alzheimer’s disease and other conditions characterized by memory impairment and cognitive problems. Actually, some compounds able to activate CAs have been identified and proposed to potentially resolve problems related to neurodegeneration. This review reports on the primary literature regarding the potential of CA activators for treating neurodegeneration-related diseases. Full article

(This article belongs to the Special Issue Carbonic Anhydrases-Chemistry and Biomedical Applications)

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