Chemical Science p. 3573 - 3585 (2019)
Update date:2022-08-04
Topics:
Uhlenbrock, Niklas
Smith, Steven
Weisner, J?rn
Landel, Ina
Lindemann, Marius
Le, Thien Anh
Hardick, Julia
Gontla, Rajesh
Scheinpflug, Rebekka
Czodrowski, Paul
Janning, Petra
Depta, Laura
Quambusch, Lena
Müller, Matthias P.
Engels, Bernd
Rauh, Daniel
The Ser/Thr kinase Akt (Protein Kinase B/PKB) is a master switch in cellular signal transduction pathways. Its downstream signaling influences cell proliferation, cell growth, and apoptosis, rendering Akt a prominent drug target. The unique activation mechanism of Akt involves a change of the relative orientation of its N-terminal pleckstrin homology (PH) and the kinase domain and makes this kinase suitable for highly specific allosteric modulation. Here we present a unique set of crystal structures of covalent-allosteric interdomain inhibitors in complex with full-length Akt and report the structure-based design, synthesis, biological and pharmacological evaluation of a focused library of these innovative inhibitors.
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Doi:10.1039/c0dt00437e
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