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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.accessioned2020-12-21T04:15:32Z
dc.date.available2020-12-21T04:15:32Z
dc.date.issued2017-02-15
dc.identifierpii: S0960-894X(16)31336-1
dc.identifier.citationSpicer, J. A., Miller, C. K., O'Connor, P. D., Jose, J., Huttunen, K. M., Jaiswal, J. K., Denny, W. A., Akhlaghi, H., Browne, K. A. & Trapani, J. A. (2017). Benzenesulphonamide inhibitors of the cytolytic protein perforin. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 27 (4), pp.1050-1054. https://doi.org/10.1016/j.bmcl.2016.12.057.
dc.identifier.issn0960-894X
dc.identifier.urihttp://hdl.handle.net/11343/257547
dc.description.abstractThe pore-forming protein perforin is a key component of mammalian cell-mediated immunity and essential to the pathway that allows elimination of virus-infected and transformed cells. Perforin activity has also been implicated in certain auto-immune conditions and therapy-induced conditions such as allograft rejection and graft versus host disease. An inhibitor of perforin activity could be used as a highly specific immunosuppressive treatment for these conditions, with reduced side-effects compared to currently accepted therapies. Previously identified first-in-class inhibitors based on a 2-thioxoimidazolidin-4-one core show suboptimal physicochemical properties and toxicity toward the natural killer (NK) cells that secrete perforin in vivo. The current benzenesulphonamide-based series delivers a non-toxic bioisosteric replacement possessing improved solubility.
dc.languageEnglish
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD
dc.rights.urihttps://creativecommons.org/licenses/by/4.0
dc.titleBenzenesulphonamide inhibitors of the cytolytic protein perforin
dc.typeJournal Article
dc.identifier.doi10.1016/j.bmcl.2016.12.057
melbourne.affiliation.departmentSir Peter MacCallum Department of Oncology
melbourne.source.titleBioorganic and Medicinal Chemistry Letters
melbourne.source.volume27
melbourne.source.issue4
melbourne.source.pages1050-1054
dc.rights.licenseCC BY
melbourne.elementsid1179873
melbourne.contributor.authorTrapani, Joseph
dc.identifier.eissn1464-3405
melbourne.accessrightsOpen Access


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