Covalent allosteric inhibitors of Akt generated using a click fragment approach

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dc.contributor.authorWesthuizen, Leandi van der
dc.contributor.authorWeisner, Jörn
dc.contributor.authorTaher, Abu
dc.contributor.authorLandel, Ina
dc.contributor.authorQuambusch, Lena
dc.contributor.authorLindemann, Marius
dc.contributor.authorUhlenbrock, Niklas
dc.contributor.authorMüller, Matthias P.
dc.contributor.authorGreen, Ivan R.
dc.contributor.authorPelly, Stephen C.
dc.contributor.authorRauh, Daniel
dc.contributor.authorOtterlo, Willem A. L. van
dc.date.accessioned2024-03-04T14:59:07Z
dc.date.available2024-03-04T14:59:07Z
dc.date.issued2022-02-16
dc.description.abstractAkt is a protein kinase that has been implicated in the progression of cancerous tumours. A number of covalent allosteric Akt inhibitors are known, and based on these scaffolds, a small library of novel potential covalent allosteric imidazopyridine-based inhibitors was designed. The envisaged compounds were synthesised, with click chemistry enabling a modular approach to a number of the target compounds. The binding modes, potencies and antiproliferative activities of these synthesised compounds were explored, thereby furthering the structure activity relationship knowledge of this class of Akt inhibitors. Three novel covalent inhibitors were identified, exhibiting moderate activity against Akt1 and various cancer cell lines, potentially paving the way for future covalent allosteric inhibitors with improved properties.en
dc.identifier.urihttp://hdl.handle.net/2003/42375
dc.identifier.urihttp://dx.doi.org/10.17877/DE290R-24212
dc.language.isoende
dc.relation.ispartofseriesChemMedChem;17(10)
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/de
dc.subjectAkt kinaseen
dc.subjectcovalent allosteric inhibitorsen
dc.subjectimidazopyridinesen
dc.subjectclick chemistryen
dc.subjectfragmentsen
dc.subject.ddc570
dc.subject.ddc540
dc.subject.rswkProtein-Serin-Threonin-Kinasende
dc.subject.rswkAllosterische Kontrollede
dc.subject.rswkImidazopyridinede
dc.subject.rswkClick-Chemiede
dc.subject.rswkInhibitorde
dc.titleCovalent allosteric inhibitors of Akt generated using a click fragment approachen
dc.typeTextde
dc.type.publicationtypeResearchArticlede
dcterms.accessRightsopen access
eldorado.secondarypublicationtruede
eldorado.secondarypublication.primarycitationL. van der Westhuizen, J. Weisner, A. Taher, I. Landel, L. Quambusch, M. Lindemann, N. Uhlenbrock, M. P. Müller, I. R. Green, S. C. Pelly, D. Rauh, W. A. L. van Otterlo, ChemMedChem 2022, 17, e202100776.de
eldorado.secondarypublication.primaryidentifierhttps://doi.org/10.1002/cmdc.202100776de

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