Advanced Search

Show simple item record

dc.contributor.authorVullo, Daniela
dc.contributor.authorIşık, Semra
dc.contributor.authorDel Prete, Sonia
dc.contributor.authorDe Luca, Viviana
dc.contributor.authorCarginale, Vincenzo
dc.contributor.authorScozzafava, Andrea
dc.contributor.authorSupuran, Claudiu
dc.contributor.authorCapasso, Clemente
dc.date.accessioned2019-11-01T11:50:21Z
dc.date.available2019-11-01T11:50:21Z
dc.date.issued2013en_US
dc.identifier.issn0960-894X
dc.identifier.issn1464-3405
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2013.01.084
dc.identifier.urihttps://hdl.handle.net/20.500.12462/9476
dc.descriptionIşık, Semra (Balikesir Author)en_US
dc.description.abstractAn alpha-carbonic anhydrase (CA, EC 4.2.1.1) has been recently cloned and characterized in the human pathogenic bacterium Vibrio cholerae, denominated VchCA (Del Prete et al. J. Med. Chem. 2012, 55, 10742). This enzyme shows a good catalytic activity for the CO2 hydration reaction, comparable to that of the human (h) isoform hCA I. Many inorganic anions and several small molecules were investigated as VchCA inhibitors. Inorganic anions such as cyanate, cyanide, hydrogen sulfide, hydrogen sulfite, and trithiocarbonate were effective VchCA inhibitors with inhibition constants in the range of 33-88 mu M. Other effective inhibitors were diethyldithiocarbamate, sulfamide, sulfamate, phenylboronic acid and phenylarsonic acid, with K(I)s of 7-43 mu M. Halides (bromide, iodide), bicarbonate and carbonate were much less effective VchCA inhibitors, with KIs in the range of 4.64-28.0 mM. The resistance of VchCA to bicarbonate inhibition may represent an evolutionary adaptation of this enzyme to living in an environment rich in this ion, such as the gastrointestinal tract, as bicarbonate is a virulence enhancer of this bacterium.en_US
dc.description.sponsorshipFP7 EU project Metoxia Ministry of National Education - Turkeyen_US
dc.language.isoengen_US
dc.publisherPergamon - Elsevier Ltden_US
dc.relation.isversionof10.1016/j.bmcl.2013.01.084en_US
dc.rightsinfo:eu-repo/semantics/embargoedAccessen_US
dc.subjectCarbonic Anhydraseen_US
dc.subjectVibrio Choleraeen_US
dc.subjectAnionen_US
dc.subjectSulfamideen_US
dc.subjectBicarbonateen_US
dc.subjectVirulence Factoren_US
dc.subjectBoronic Aciden_US
dc.titleAnion inhibition studies of the α-carbonic anhydrase from the pathogenic bacterium Vibrio choleraeen_US
dc.typearticleen_US
dc.relation.journalBioorganic and Medicinal Chemistry Lettersen_US
dc.contributor.departmentFen Edebiyat Fakültesien_US
dc.contributor.authorID0000-0003-3314-2411en_US
dc.contributor.authorID0000-0002-1842-494Xen_US
dc.contributor.authorID0000-0001-5020-3322en_US
dc.identifier.volume23en_US
dc.identifier.issue6en_US
dc.identifier.startpage1636en_US
dc.identifier.endpage1638en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US


Files in this item

Thumbnail

This item appears in the following Collection(s)

Show simple item record