| Autor: |
Siham A, Alissa, Hanan A, Alghulikah, Zeid A, ALOthman, Sameh M, Osman, Sonia, Del Prete, Clemente, Capasso, Alessio, Nocentini, Claudiu T, Supuran |
| Rok vydání: |
2019 |
| Předmět: |
|
| Zdroj: |
Journal of Enzyme Inhibition and Medicinal Chemistry |
| ISSN: |
1475-6374 |
| Popis: |
The inhibition of δ- and η-class carbonic anhydrases (CAs; EC 4.2.1.1) was poorly investigated so far. Only one δ-CA, TweCA from the diatom Thalassiosira weissflogii, and one η-CA, PfCA, from Plasmodium falciparum, have been cloned and characterised to date. To enrich δ- and η-CAs inhibition profiles, a panel of 22 phenols was investigated for TweCA and PfCA inhibition. Some derivatives showed effective, sub-micromolar inhibition of TweCA (KIs 0.81–65.4 µM) and PfCA (KIs 0.62–78.7 µM). A subset of compounds demonstrated a significant selectivity for the target CAs over the human physiologically relevant ones. This study promotes the identification of new potent and selective inhibitors of TweCA and PfCA, which could be considered as leads for finding molecular probes in the study of carbon fixation processes (in which TweCA and orthologue enzymes are involved) or drug candidates in the treatment of malaria. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
