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. Author manuscript; available in PMC: 2018 Jun 1.
Published in final edited form as: Nat Chem. 2017 Jul 31;9(12):1181–1190. doi: 10.1038/nchem.2826

Figure 4.

Figure 4

Analysis of fragment-lysine interactions. a, Heat-map showing R values for representative lysines and fragments organized by relative proteomic reactivity of the fragments (high to low, left to right) and number of fragment hits for individual lysines (high to low, top to bottom). b, Fragment SAR determined by competitive isoTOP-ABPP is recapitulated by gel-based ABPP of recombinant proteins. Left panel, heat-map depicts R values for the indicated fragment-lysine interactions determined by competitive isoTOP-ABPP. Right panel, HEK 293T cells recombinantly expressing representative liganded proteins (or the corresponding lysine-to-arginine (KR) mutants) as FLAG epitope-tagged proteins were treated with fragment electrophiles (50 μM, 1 h) followed by the indicated lysine-reactive probes and analyzed by gel-based ABPP. SIN3A corresponds to a.a. 1-400 of SIN3A.