Discovery of fully synthetic FKBP12-mTOR molecular glues

Chem. Sci., 2025, 16,4256-4263
DOI: 10.1039/D4SC06917J, Edge Article

Open Access

&nbsp This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.

Robin C. E. Deutscher, Christian Meyners, Maximilian L. Repity, Wisely Oki Sugiarto, Jürgen M. Kolos, Edvaldo V. S. Maciel, Tim Heymann, Thomas M. Geiger, Stefan Knapp, Frederik Lermyte, Felix Hausch
We discovered a fully synthetic non-degradative molecular glue for the ternary complex between FKBP12 and the FRB domain of mTOR by screening a library of FKBP12 ligands. Solving the ternary complex structure allowed significant potency enhancement.
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