Fig. 5: Programmable kinase inhibition with FKBP-dependent kinase inhibitors and RapaBlock.
From: Brain-restricted mTOR inhibition with binary pharmacology
a, Structures of GNE7915 and FK-GNE7915. b, Proposed working model for FKBP-dependent kinase inhibitors. c, Kinase inhibition in the absence or presence of supplemented 10 µM recombinant FKBP12 protein (n = 2; data are shown as individual points). d,e, RAW264.7 cells were treated with GNE7915, FK-GNE7915 and/or RapaBlock, and phospho-LRRK2 (S935) was analysed by time-resolved FRET using epitopically orthogonal antibodies for LRRK2 and p-LRRK2 (S935) (n = 3; data are presented as mean ± s.d.). See Supplementary Information for experimental details.
