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. Author manuscript; available in PMC: 2018 Dec 11.
Published in final edited form as: Nat Chem Biol. 2018 Jun 11;14(7):706–714. doi: 10.1038/s41589-018-0055-y

Figure 2. Degrader mediated BRD4 recruitment is governed by negative cooperativity.

Figure 2

(a) TR-FRET. dBET23 titrated to DDB1ΔB-CRBNSPY-BODIPY, Terbium-Streptavidin and various BRD4BD1-biotin wild type and mutant proteins. The mean peak heights for dose response curves of three independent replicates are shown as dot-plot. Data in this figure is presented as means ± s.d. (n=3). (b) Competitive binding assay for dBET1 binding to DDB1ΔB-CRBN. Increasing concentrations of dBET1 titrated to preformed DDB1ΔB-CRBN-lenalidomideAtto565 complex in presence or absence of BRD4BD1 or BRD4BD2. (c) As in b but using dBET6, (d) dBET23, or (e) dBET57. All data in this figure are independent replicates presented as means ± s.d. (n=3).