Unknown

Dataset Information

0

Discovering a new class of antifungal agents that selectively inhibits microbial carbonic anhydrases.


ABSTRACT: Infections caused by pathogens resistant to the available antimicrobial treatments represent nowadays a threat to global public health. Recently, it has been demonstrated that carbonic anhydrases (CAs) are essential for the growth of many pathogens and their inhibition leads to growth defects. Principal drawbacks in using CA inhibitors (CAIs) as antimicrobial agents are the side effects due to the lack of selectivity toward human CA isoforms. Herein we report a new class of CAIs, which preferentially interacts with microbial CA active sites over the human ones. The mechanism of action of these inhibitors was investigated against an important fungal pathogen, Cryptococcus neoformans, revealing that they are also able to inhibit CA in microbial cells growing in vitro. At our best knowledge, this is the first report on newly designed synthetic compounds selectively targeting ?-CAs and provides a proof of concept of microbial CAs suitability as an antimicrobial drug target.

SUBMITTER: Annunziato G 

PROVIDER: S-EPMC6179086 | biostudies-literature | 2018 Dec

REPOSITORIES: biostudies-literature

altmetric image

Publications

Discovering a new class of antifungal agents that selectively inhibits microbial carbonic anhydrases.

Annunziato Giannamaria G   Giovati Laura L   Angeli Andrea A   Pavone Marialaura M   Del Prete Sonia S   Pieroni Marco M   Capasso Clemente C   Bruno Agostino A   Conti Stefania S   Magliani Walter W   Supuran Claudiu T CT   Costantino Gabriele G  

Journal of enzyme inhibition and medicinal chemistry 20181201 1


Infections caused by pathogens resistant to the available antimicrobial treatments represent nowadays a threat to global public health. Recently, it has been demonstrated that carbonic anhydrases (CAs) are essential for the growth of many pathogens and their inhibition leads to growth defects. Principal drawbacks in using CA inhibitors (CAIs) as antimicrobial agents are the side effects due to the lack of selectivity toward human CA isoforms. Herein we report a new class of CAIs, which preferent  ...[more]

Similar Datasets

| S-EPMC6690855 | biostudies-literature
| S-EPMC2918522 | biostudies-literature
| S-EPMC6273118 | biostudies-literature
| S-EPMC8122340 | biostudies-literature
| S-EPMC6187404 | biostudies-literature
| S-EPMC4519908 | biostudies-literature
| S-EPMC4360143 | biostudies-literature
| S-EPMC9848372 | biostudies-literature
| S-EPMC4162934 | biostudies-literature
| S-EPMC8741243 | biostudies-literature