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Zhichao Zhang, Yan Zhao, Ting Song, Yubo Liu, Xiangqian Li, Pengchen Su and Shenghui Xie Study of Binding Thermodynamics in the Optimization of BH3 Mimetics Chemical Biology & Drug Design 82

Version of Record online: 10 SEP 2013 | DOI: 10.1111/cbdd.12161

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Isothermal titration calorimetry was used to evaluate the optimization of B-cell lymphoma 2 homology domain 3-mimetics (compounds 16) from a thermodynamic perspective. Owing to 16 overcoming enthalpy-entropy compensation, the affinities of them improved gradually. Comparing 2 with 1, the enthalpy gain indicated the formation of an additional hydrogen bond to myeloid cell leukemia sequence 1 protein.

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