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dc.contributor.authorLindenmann, Urs-
dc.contributor.authorBrand, Michael-
dc.contributor.authorGall, Flavio-
dc.contributor.authorFrasson, David-
dc.contributor.authorHunziker, Lukas-
dc.contributor.authorKroslakova, Ivana-
dc.contributor.authorSievers, Martin-
dc.contributor.authorRiedl, Rainer-
dc.date.accessioned2021-02-18T13:45:44Z-
dc.date.available2021-02-18T13:45:44Z-
dc.date.issued2020-02-21-
dc.identifier.issn1860-7179de_CH
dc.identifier.issn1860-7187de_CH
dc.identifier.urihttps://digitalcollection.zhaw.ch/handle/11475/21813-
dc.description.abstractSentrin-specific proteases (SENPs) are responsible for the maturation of small ubiquitin-like modifiers (SUMOs) and the deconjugation of SUMOs from their substrate proteins. Studies on prostate cancer revealed an overexpression of SENP1, which promotes prostate cancer progression as well as metastasis. Therefore, SENP1 has been identified as a novel drug target against prostate cancer. Herein, we report the discovery and biological evaluation of potent and selective SENP1 inhibitors. A structure-activity relationship (SAR) of the newly identified pyridone scaffold revealed allosteric inhibitors with very attractive in vitro ADMET properties regarding plasma binding and plasma stability for this challenging target. This study also emphasizes the importance of biochemical mode of inhibition studies for de novo designed inhibitors.de_CH
dc.language.isoende_CH
dc.publisherWileyde_CH
dc.relation.ispartofChemMedChemde_CH
dc.rightsLicence according to publishing contractde_CH
dc.subjectDrug designde_CH
dc.subjectDrug discoveryde_CH
dc.subjectInhibitorsde_CH
dc.subjectMedicinal chemistryde_CH
dc.subjectStructure-activity relationshipde_CH
dc.subject.ddc615: Pharmakologie und Therapeutikde_CH
dc.titleDiscovery of a class of potent and selective non‐competitive sentrin‐specific protease 1 inhibitorsde_CH
dc.typeBeitrag in wissenschaftlicher Zeitschriftde_CH
dcterms.typeTextde_CH
zhaw.departementLife Sciences und Facility Managementde_CH
zhaw.organisationalunitInstitut für Chemie und Biotechnologie (ICBT)de_CH
dc.identifier.doi10.1002/cmdc.202000067de_CH
dc.identifier.pmid32083799de_CH
zhaw.funding.euNode_CH
zhaw.issue8de_CH
zhaw.originated.zhawYesde_CH
zhaw.pages.end679de_CH
zhaw.pages.start675de_CH
zhaw.publication.statuspublishedVersionde_CH
zhaw.volume15de_CH
zhaw.publication.reviewPeer review (Publikation)de_CH
zhaw.author.additionalNode_CH
zhaw.display.portraitYesde_CH
Appears in collections:Publikationen Life Sciences und Facility Management

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