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

oleh: 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
Diterbitkan: Nature Portfolio 2021-09-01

Deskripsi

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