| Literature DB >> 33472446 |
Alessandro Bonardi1,2, Alessio Nocentini1,2, Sameh Mohamed Osman3, Fatmah Ali Alasmary3, Tahani Mazyad Almutairi3, Dalal Saied Abdullah3, Paola Gratteri1,2, Claudiu T Supuran2.
Abstract
The binding mode of aromatic sulphonamides and clinically licenced drugs to the three carbonic anhydrase (CA, EC 4.2.1.1) isoforms from the human pathogen V. cholerae was here thouroghly characterised by a joint docking and molecular dynamics in silico protocol. In fact, VchCA, VchCAβ, and VchCAγ are crucial in the pathogen life cycle and growth and represent innovative targets to fight V. cholerae proliferation overcoming the spreading chemoresistance to the available drugs. A set of 40 sulphonamides/sulfamates VchCAs inhibitors was studied using the proteins homology built 3 D models unveiling the key and stable interactions responsible for a potent CA inhibition. This study has the aim to offer insights and guidelines for the future rational design of potent and selective inhibitors targeting CA isoforms from V. cholerae or other human pathogens.Entities:
Keywords: MD; Resistance; inhibition; metalloenzyme; virulence
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Year: 2021 PMID: 33472446 PMCID: PMC7822066 DOI: 10.1080/14756366.2020.1862102
Source DB: PubMed Journal: J Enzyme Inhib Med Chem ISSN: 1475-6366 Impact factor: 5.051