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Five- and Six-Membered Nitrogen-Containing Compounds as Selective Carbonic Anhydrase Activators

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dc.contributor.authorMollica, Adriano
dc.contributor.authorMacedonio, Giorgia
dc.contributor.authorStefanucci, Azzurra
dc.contributor.authorCarradori, Simone
dc.contributor.authorAkdemir, ATİLLA
dc.contributor.authorANGELI, Andrea
dc.contributor.authorSupuran, Claudiu T.
dc.contributor.institutionauthorAKDEMİR, ATİLLA
dc.date.accessioned2019-10-05T14:23:22Z
dc.date.available2019-10-05T14:23:22Z
dc.date.issued2017-12-01
dc.description.abstractIt has been proven that specific isoforms of human carbonic anhydrase (hCA) are able to fine-tune physiological pathways connected to signal processing, and that decreased CAs expression negatively influences cognition, leading to mental retardation, Alzheimer’s disease, and aging-related cognitive dysfunctions. For this reason, a small library of natural and synthetic nitrogen containing cyclic derivatives was assayed as activators of four human isoforms of carbonic anhydrase (hCA I, II, IV and VII). Most of the compounds activated hCA I, IV and VII in the micromolar range, with KAs ranging between 3.46 and 80.5 µM, whereas they were not active towards hCA II (KAs > 100 µM). Two natural compounds, namely L-(+)-ergothioneine (1) and melatonin (2), displayed KAs towards hCA VII in the nanomolar range after evaluation by a CO2 hydration method in vitro, showing a rather efficient and selective activation profile with respect to histamine, used as a reference compound. Corroborated with the above in vitro findings, a molecular modelling in silico approach has been performed to correlate these biological data, and to elucidate the binding interaction of these activators within the enzyme active site.en
dc.identifier10.1021/jm400414j
dc.identifier.citationMollica A., Macedonio G., Stefanucci A., Carradori S., Akdemir A., ANGELI A., Supuran C. T. , -Five- and Six-Membered Nitrogen-Containing Compounds as Selective Carbonic Anhydrase Activators-, MOLECULES, cilt.22, 2017
dc.identifier.pubmed29232847
dc.identifier.urihttps://hdl.handle.net/20.500.12645/3743
dc.language.isoen
dc.rightsinfo:eu-repo/semantics/openAccessen
dc.titleFive- and Six-Membered Nitrogen-Containing Compounds as Selective Carbonic Anhydrase Activators
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameJournal of medicinal chemistry
local.avesis.id5ac8f781-76ba-44a4-83c4-dd99894eac35
local.avesis.response3613
local.publication.goal03 - Sağlık ve Kaliteli Yaşam
relation.isAuthorOfPublication19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isAuthorOfPublication.latestForDiscovery19bc513a-c695-4e72-ba1d-83b8d6c574c8
relation.isGoalOfPublication9c198c48-b603-4e2f-8366-04edcfc1224c
relation.isGoalOfPublication.latestForDiscovery9c198c48-b603-4e2f-8366-04edcfc1224c
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