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Study on Daptomycin as a New Trypsin Activator |
YANG Tian-ran, WU Shi-jie, XIN Ming-xiu |
College of Life Sciences, Beijing Normal University, Beijing Key Laboratory of Genetically Engineered Drug and Biotechnology, Beijing 100875, China |
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Abstract The activity of trypsin was increased 32.92% on average when the amount of substance rate between trypsin and daptomycin is 34.05, which indicated that daptomycin is a new trypsin activator. Daptomycin-trypsin and daptomycin-trypsin-substrate complex were studied by the molecular docking, and isothermal titration calorimetry (ITC) was used to support the result of molecular docking. It showed that daptomycin was close to the activity center of trypsin, and the R group of daptomycin was interacted with histidine-57 of trypsin, and this histidine-57 located in the activity center of the enzyme. The complex structure between enzyme and substrate is more stable when the daptomycin is presence, which is beneficial to the catalytic effect. The ITC results demonstrated that a daptomycin binding site was located in trypsin, and the dissociation constant Kd is 17.83 μM, molar combustion enthalpy △H is 237.9±28.17 cal/mol, molar binding entropy △S is 22.5 cal/mol/deg, and all the results support the molecular docking results. It indicated that daptomycin is a new trypsin activator and it will have application in proteomics and other fields.
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Received: 13 April 2017
Published: 25 October 2017
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