Next Article in Journal
Inhibitory Effects of Ginsenoside Rb1 on Early Atherosclerosis in ApoE-/- Mice via Inhibition of Apoptosis and Enhancing Autophagy
Previous Article in Journal
In Silico Analysis of Bioactive Peptides Released from Giant Grouper (Epinephelus lanceolatus) Roe Proteins Identified by Proteomics Approach
Previous Article in Special Issue
Cancer Drug Development of Carbonic Anhydrase Inhibitors beyond the Active Site
Article Menu

Export Article

Open AccessReview
Molecules 2018, 23(11), 2911; https://doi.org/10.3390/molecules23112911

Carbonic Anhydrase Inhibitors as Novel Drugs against Mycobacterial β-Carbonic Anhydrases: An Update on In Vitro and In Vivo Studies

1
Faculty of Medicine and Health Technology, University of Tampere, 33014 Tampere, Finland
2
Institut des Biomolécules Max Mousseron (IBMM) UMR 5247 CNRS, ENSCM, Université de Montpellier, 34296 Montpellier CEDEX 05, France
3
Neurofarba Department, Sezione di Chimica Farmaceutica e Nutraceutica, Università degli Studi di Firenze, 50019 Sesto Fiorentino (Firenze), Italy
4
Oral and Maxillofacial Unit, Tampere University Hospital, 33521 Tampere, Finland
5
Fimlab Ltd. and Tampere University Hospital, 33520 Tampere, Finland
*
Author to whom correspondence should be addressed.
Received: 23 October 2018 / Revised: 5 November 2018 / Accepted: 6 November 2018 / Published: 8 November 2018
(This article belongs to the Special Issue Metalloenzyme Inhibitors and Activators)
Full-Text   |   PDF [2291 KB, uploaded 8 November 2018]   |  

Abstract

Mycobacteria cause a variety of diseases, such as tuberculosis, leprosy, and opportunistic diseases in immunocompromised people. The treatment of these diseases is problematic, necessitating the development of novel treatment strategies. Recently, β-carbonic anhydrases (β-CAs) have emerged as potential drug targets in mycobacteria. The genomes of mycobacteria encode for three β-CAs that have been cloned and characterized from Mycobacterium tuberculosis (Mtb) and the crystal structures of two of the enzymes have been determined. Different classes of inhibitor molecules against Mtb β-CAs have subsequently been designed and have been shown to inhibit these mycobacterial enzymes in vitro. The inhibition of these centrally important mycobacterial enzymes leads to reduced growth of mycobacteria, lower virulence, and impaired biofilm formation. Thus, the inhibition of β-CAs could be a novel approach for developing drugs against the severe diseases caused by pathogenic mycobacteria. In the present article, we review the data related to in vitro and in vivo inhibition studies in the field. View Full-Text
Keywords: mycobacterial diseases; β-carbonic anhydrases; Mycobacterium tuberculosis; drug targets; carbonic anhydrase inhibitors; in vivo inhibition; in vitro inhibition mycobacterial diseases; β-carbonic anhydrases; Mycobacterium tuberculosis; drug targets; carbonic anhydrase inhibitors; in vivo inhibition; in vitro inhibition
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
SciFeed

Share & Cite This Article

MDPI and ACS Style

Aspatwar, A.; Winum, J.-Y.; Carta, F.; Supuran, C.T.; Hammaren, M.; Parikka, M.; Parkkila, S. Carbonic Anhydrase Inhibitors as Novel Drugs against Mycobacterial β-Carbonic Anhydrases: An Update on In Vitro and In Vivo Studies. Molecules 2018, 23, 2911.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top