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dc.contributor.authorSpicer JA
dc.contributor.authorMiller CK
dc.contributor.authorO'Connor PD
dc.contributor.authorJose J
dc.contributor.authorHuttunen KM
dc.contributor.authorJaiswal JK
dc.contributor.authorDenny WA
dc.contributor.authorAkhlaghi H
dc.contributor.authorBrowne KA
dc.contributor.authorTrapani JA
dc.date.accessioned2017-09-27T12:30:38Z
dc.date.available2017-09-27T12:30:38Z
dc.date.issued2017
dc.identifier.urihttps://erepo.uef.fi/handle/123456789/4340
dc.description.abstractThe structure-activity relationships for a series of arylsulphonamide-based inhibitors of the pore-forming protein perforin have been explored. Perforin is a key component of the human immune response, however inappropriate activity has also been implicated in certain auto-immune and therapy-induced conditions such as allograft rejection and graft versus host disease. Since perforin is expressed exclusively by cells of the immune system, inhibition of this protein would be a highly selective strategy for the immunosuppressive treatment of these disorders. Compounds from this series were demonstrated to be potent inhibitors of the lytic action of both isolated recombinant perforin and perforin secreted by natural killer cells in vitro. Several potent and soluble examples were assessed for in vivo pharmacokinetic properties and found to be suitable for progression to an in vivo model of transplant rejection.en
dc.language.isoENen
dc.publisherElsevier BVen
dc.relation.ispartofseriesEUROPEAN JOURNAL OF MEDICINAL CHEMISTRYen
dc.relation.urihttp://dx.doi.org/10.1016/j.ejmech.2017.05.048en
dc.rightsCC BY-NC-ND https://creativecommons.org/licenses/by-nc-nd/4.0/en
dc.subjectPerforinen
dc.subjectPerforin inhibitoren
dc.subjectArylsulphonamideen
dc.subjectBioisostereen
dc.subjectImmunosuppressanten
dc.titleSubstituted arylsulphonamides as inhibitors of perforin-mediated lysisen
dc.description.versionfinal draften
dc.contributor.departmentSchool of Pharmacy, Activitiesen
uef.solecris.id48034669en
dc.type.publicationinfo:eu-repo/semantics/articleen
dc.rights.accessrights© Authorsen
dc.relation.doi10.1016/j.ejmech.2017.05.048en
dc.description.reviewstatuspeerRevieweden
dc.format.pagerange139-155en
dc.relation.issn0223-5234en
dc.relation.volume137en
dc.rights.accesslevelopenAccessen
dc.type.okmA1en
dc.type.versioninfo:eu-repo/semantics/acceptedVersionen


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