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. Author manuscript; available in PMC: 2015 Jun 7.
Published in final edited form as: Science. 2014 Oct 16;346(6209):638–641. doi: 10.1126/science.1249830

Fig. 3. Bumped ligand ET binds to engineered L/A bromodomains with high selectivity.

Fig. 3

(A) Thermal stabilization (ΔTm, in degrees Celsius) of WT Brd2 bromodomains and their L/A mutants by I-BET, ME, and ET measured by means of DSF. The data shown are mean ± SD of three measurements. (B) Dissociation constants (Kd, in nanomolar) determined by means of ITC for I-BET binding to WT and for ME and ET binding to WT and L/A mutant Brd2 bromodomains. The error bars reflect the quality of the fit between the nonlinear least-squares curve and the experimental points. (C and D) Cocrystal structures of Brd2(2)L383A (green, surface representation) in complex with ME [(C) stick, yellow carbons] and ET [(D) stick, pink carbons].The L/A mutation is shown in red, and A383 is shown as stick, green carbons. (E and F) Affinity profile (Kd, in nanomolar) of ET binding to (E) wild-type and (F) L/A mutant BET bromodomains measured by means of ITC.