PMID- 30413024
OWN - NLM
STAT- MEDLINE
DCOM- 20190114
LR  - 20190114
IS  - 1420-3049 (Electronic)
IS  - 1420-3049 (Linking)
VI  - 23
IP  - 11
DP  - 2018 Nov 8
TI  - Carbonic Anhydrase Inhibitors as Novel Drugs against Mycobacterial beta-Carbonic 
      Anhydrases: An Update on In Vitro and In Vivo Studies.
LID - 10.3390/molecules23112911 [doi]
LID - 2911
AB  - 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, beta-carbonic anhydrases (beta-CAs) have emerged as potential 
      drug targets in mycobacteria. The genomes of mycobacteria encode for three beta-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 beta-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 beta-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.
FAU - Aspatwar, Ashok
AU  - Aspatwar A
AUID- ORCID: 0000-0002-6938-7835
AD  - Faculty of Medicine and Health Technology, University of Tampere, 33014 Tampere, 
      Finland. ashok.aspatwar@staff.uta.fi.
FAU - Winum, Jean-Yves
AU  - Winum JY
AUID- ORCID: 0000-0003-3197-3414
AD  - Institut des Biomolecules Max Mousseron (IBMM) UMR 5247 CNRS, ENSCM, Universite 
      de Montpellier, 34296 Montpellier CEDEX 05, France. 
      Jean-yves.winum@umontpellier.fr.
FAU - Carta, Fabrizio
AU  - Carta F
AUID- ORCID: 0000-0002-1141-6146
AD  - Neurofarba Department, Sezione di Chimica Farmaceutica e Nutraceutica, Universita 
      degli Studi di Firenze, 50019 Sesto Fiorentino (Firenze), Italy. 
      fabrizio.carta@unifi.it.
FAU - Supuran, Claudiu T
AU  - Supuran CT
AUID- ORCID: 0000-0003-4262-0323
AD  - Neurofarba Department, Sezione di Chimica Farmaceutica e Nutraceutica, Universita 
      degli Studi di Firenze, 50019 Sesto Fiorentino (Firenze), Italy. 
      claudiu.supuran@unifi.it.
FAU - Hammaren, Milka
AU  - Hammaren M
AUID- ORCID: 0000-0001-9076-8782
AD  - Faculty of Medicine and Health Technology, University of Tampere, 33014 Tampere, 
      Finland. milka.hammaren@staff.uta.fi.
FAU - Parikka, Mataleena
AU  - Parikka M
AD  - Faculty of Medicine and Health Technology, University of Tampere, 33014 Tampere, 
      Finland. mataleena.parikka@staff.uta.fi.
AD  - Oral and Maxillofacial Unit, Tampere University Hospital, 33521 Tampere, Finland. 
      mataleena.parikka@staff.uta.fi.
FAU - Parkkila, Seppo
AU  - Parkkila S
AUID- ORCID: 0000-0001-7323-8536
AD  - Faculty of Medicine and Health Technology, University of Tampere, 33014 Tampere, 
      Finland. seppo.parkkila@staff.uta.fi.
AD  - Fimlab Ltd. and Tampere University Hospital, 33520 Tampere, Finland. 
      seppo.parkkila@staff.uta.fi.
LA  - eng
GR  - None/Suomen Kulttuurirahasto/
GR  - None/Tampereen Tuberkuloosisaatio/
GR  - None/Jane ja Aatos Erkon Saatio/
PT  - Journal Article
PT  - Review
DEP - 20181108
PL  - Switzerland
TA  - Molecules
JT  - Molecules (Basel, Switzerland)
JID - 100964009
RN  - 0 (Antitubercular Agents)
RN  - 0 (Bacterial Proteins)
RN  - 0 (Carbonic Anhydrase Inhibitors)
RN  - EC 4.2.1.- (Carbonic Anhydrase I)
SB  - IM
MH  - Antitubercular Agents/chemistry/*pharmacology
MH  - Bacterial Proteins/antagonists & inhibitors/chemistry/genetics
MH  - Biofilms/drug effects
MH  - Carbonic Anhydrase I/antagonists & inhibitors/chemistry/*genetics
MH  - Carbonic Anhydrase Inhibitors/chemistry/*pharmacology
MH  - Models, Molecular
MH  - Mycobacterium tuberculosis/drug effects/genetics/*growth & development
MH  - Structure-Activity Relationship
MH  - Virulence/drug effects
PMC - PMC6278287
OTO - NOTNLM
OT  - Mycobacterium tuberculosis
OT  - carbonic anhydrase inhibitors
OT  - drug targets
OT  - in vitro inhibition
OT  - in vivo inhibition
OT  - mycobacterial diseases
OT  - beta-carbonic anhydrases
COIS- The authors declare no conflict of interest.
EDAT- 2018/11/11 06:00
MHDA- 2019/01/15 06:00
PMCR- 2018/11/08
CRDT- 2018/11/11 06:00
PHST- 2018/10/23 00:00 [received]
PHST- 2018/11/05 00:00 [revised]
PHST- 2018/11/06 00:00 [accepted]
PHST- 2018/11/11 06:00 [entrez]
PHST- 2018/11/11 06:00 [pubmed]
PHST- 2019/01/15 06:00 [medline]
PHST- 2018/11/08 00:00 [pmc-release]
AID - molecules23112911 [pii]
AID - molecules-23-02911 [pii]
AID - 10.3390/molecules23112911 [doi]
PST - epublish
SO  - Molecules. 2018 Nov 8;23(11):2911. doi: 10.3390/molecules23112911.