An inhibition model of BPTI to unlinked dengue virus NS2B-NS3 protease |
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| Authors: | Hua Li Lei Zhu Shulin Hou Jing Yang Junfeng Wang Jinsong Liu |
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| Institution: | 1. Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China;2. High Magnetic Field Laboratory, Chinese Academy of Sciences, Hefei 230031, China;3. Graduate University of Chinese Academy of Sciences, Beijing 100049, China |
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| Abstract: | One approach to treating the dengue virus infection is to inhibit its NS2B-NS3 protease that plays a vital role in virus maturation. However, the lack of structural information on the active conformation of the protease hindered related drug design. With a co-expression system, we obtained the active two-component protease in its unlinked form. BPTI shows strong competitive inhibitory activity (Ki = 6.5 nM) against this unlinked protease, which adopts a closed conformation. Based on the biochemical and NMR perturbation information, an inhibition model of BPTI to NS2B-NS3 protease is proposed. |
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| Keywords: | Dengue virus NS2B-NS3 protease Bovine pancreatic trypsin inhibitor NMR spectroscopy Closed/active conformation |
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