Fig. 2
In vitro FKBP12 labelling with LDNASA reagents 1–3. a Molecular structures of LDNASA reagents 1–3. b MALDI-TOF mass analysis of FKBP12 labelling by 1 in the absence or presence of rapamycin (Rap). Reaction conditions: 5 µM FKBP12, 10 µM 1, 100 µM Rap, 50 mM HEPES buffer, pH 7.2, 37 °C. o, native FKBP12 (M w : 11 914); *, single-labelled FKBP12 (M w : 12 140); **, double-labelled FKBP12 (M w : 12 366). c Initial rates (M min−1) of FKBP12 labelling by 1–3. The initial rates were estimated from the time courses of the reaction yields (inset). n.d., not detected. d The crystal structure of the FKBP12-SLF complex (PDB:1FKG). Lys44, the major labelling site with 1, is coloured in red. The SLF ligand is shown as a green stick. Lys34 was also identified as the second (minor) labelling site (see Supplementary Figure 5)
