Please use this identifier to cite or link to this item: https://doi.org/10.1021/jm8005433
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dc.titleStructure-activity relationship studies of phenanthridine-based Bcl-X L inhibitors
dc.contributor.authorBernardo, P.H.
dc.contributor.authorWan, K.-F.
dc.contributor.authorSivaraman, T.
dc.contributor.authorXu, J.
dc.contributor.authorMoore, F.K.
dc.contributor.authorHung, A.W.
dc.contributor.authorMok, H.Y.K.
dc.contributor.authorYu, V.C.
dc.contributor.authorChai, C.L.L.
dc.date.accessioned2014-10-27T08:40:53Z
dc.date.available2014-10-27T08:40:53Z
dc.date.issued2008-11-13
dc.identifier.citationBernardo, P.H., Wan, K.-F., Sivaraman, T., Xu, J., Moore, F.K., Hung, A.W., Mok, H.Y.K., Yu, V.C., Chai, C.L.L. (2008-11-13). Structure-activity relationship studies of phenanthridine-based Bcl-X L inhibitors. Journal of Medicinal Chemistry 51 (21) : 6699-6710. ScholarBank@NUS Repository. https://doi.org/10.1021/jm8005433
dc.identifier.issn00222623
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/101778
dc.description.abstractDespite their structural similarities, the natural products chelerythrine (5) and sanguinarine (6) target different binding sites on the pro-survival Bcl-XL protein. This paper details the synthesis of phenanthridine-based analogues of the natural products that were used to probe this difference in binding profiles. The inhibitory constants for these compounds were then measured in a fluorescence polarization assay against Bcl-XL and the tagged Bak-BH3 peptide. The results led to structure-activity relationship studies, which identified the structural motifs required for binding-site specificity as well as inhibitory activity. We also identified synthetic analogues of the natural products that display similar binding modes but with more potent IC50 values. © 2008 American Chemical Society.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1021/jm8005433
dc.sourceScopus
dc.typeArticle
dc.contributor.departmentBIOLOGICAL SCIENCES
dc.description.doi10.1021/jm8005433
dc.description.sourcetitleJournal of Medicinal Chemistry
dc.description.volume51
dc.description.issue21
dc.description.page6699-6710
dc.description.codenJMCMA
dc.identifier.isiut000260730900013
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