Fig. 10. PrOF NMR studies for screening against bromodomains. (A) PrOF NMR spectra of various 5FW-labeled bromodomains. The tryptophan reporter residue located in the WPF shelf denoted by asterisk. (adapted from ref. 131 with permission from MDPI, copyright 2020). (B) The tryptophan reporter residue (5FW) in bromodomains is adjacent to the acetyl lysine (Kac) binding site. (PDB:3QZS, pending) (C) PrOF NMR titration of a fragment mixture that has hits for both 5FW-BPTF and 5FW PfGCN5 in a dual protein mixture (adapted from ref. 131 with permission from MDPI, copyright 2020). (D) PrOF NMR titration with fragment hit 1 with 5FW-BRD4 D1 and Kd determination from W81. (adapted from ref. 133 with permission from American Chemical Society, copyright 2019). (E) PrOF NMR titration with deconstructed fragment F6 (from parent molecule (S)-AU1) with 5FW-BPTFand Kd determination from W2950. (adapted from ref. 136 with permission from Royal Society of Chemistry, copyright 2019).
