Cellular model system to dissect the isoform-selectivity of Akt inhibitors

Elucidating specific effects of protein kinase Akt isoforms remains challenging. Here, the authors establish an Akt isoform-dependent cellular model system and use it, together with X-ray crystallography and structure-based ligand design, to develop isoform-selective covalent-allosteric Akt inhibito...

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Auteurs principaux: Lena Quambusch, Laura Depta, Ina Landel, Melissa Lubeck, Tonia Kirschner, Jonas Nabert, Niklas Uhlenbrock, Jörn Weisner, Michael Kostka, Laura M. Levy, Carsten Schultz-Fademrecht, Franziska Glanemann, Kristina Althoff, Matthias P. Müller, Jens T. Siveke, Daniel Rauh
Format: article
Langue:EN
Publié: Nature Portfolio 2021
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Accès en ligne:https://doaj.org/article/e9d5b9b56b6e4d8f9a3489c70c876e8e
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Résumé:Elucidating specific effects of protein kinase Akt isoforms remains challenging. Here, the authors establish an Akt isoform-dependent cellular model system and use it, together with X-ray crystallography and structure-based ligand design, to develop isoform-selective covalent-allosteric Akt inhibitors