[논문]Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris

Nguyen, Thi Thanh Hanh; Woo, Hye-Jin; Kang, Hee-Kyoung; Nguyen, Van Dao; Kim, Young-Min; Kim, Do-Won; Ahn, Sul-Ah; Xia, Yongmei; Kim, Doman

doi:10.1007/s10529-011-0845-8

Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris 원문보기

Biotechnology letters. : a monthly journal for the rapid communication of results and developments in all aspects of biotechnology, v.34 no.5, 2012년, pp.831 - 838

Nguyen, Thi Thanh Hanh (School of Biological Sciences and Technology and the Research Institute for Catalysis, Chonnam National University, 77 Yongbong-ro, Buk-gu, Gwangju, 500-757 Republic of Korea) , Woo, Hye-Jin (School of Biological Sciences and Technology and the Research Institute for Catalysis, Chonnam National University, 77 Yongbong-ro, Buk-gu, Gwangju, 500-757 Republic of Korea) , Kang, Hee-Kyoung (School of Biological Sciences and Technology and the Research Institute for Catalysis, Chonnam National University, 77 Yongbong-ro, Buk-gu, Gwangju, 500-757 Republic of Korea) , Nguyen, Van Dao (Biotechnology Faculty, Hanoi Open University, 46 Ta Quang Buu street, Hai Ba Trung District, Hanoi, Vietnam) , Kim, Young-Min (Eco-Friendly Biomaterial Research Center, Korea Research Institute of Bioscience and Biotechnology, Jeongeup, 580-185 Republic of Korea) , Kim, Do-Won (Department of Physics, Gangeung-wonju National University, Gangneung, 210-702 Republic of Korea) , Ahn, Sul-Ah (Global Science Experimental Data Hub Center, Korea Institute of Science and Technology Information, Daejeon, 805-306 Republ) , Xia, Yongmei , Kim, Doman

Abstract ▼ AI-Helper

The 3C-like protease (3CLpro) of severe acute respiratory syndrome associated coronavirus (SARS-CoV) is vital for SARS-CoV replication and is a promising drug target. Recombinant 3CLpro was expressed in Pichia pastoris GS115 as a 42 kDa protein that displayed a Km of 15 ± 2 μM with Dabcyl-KTSAVLQSGFRKME-Edans as substrate. Purified 3CLpro was used for inhibition and kinetic assays with seven flavonoid compounds. The IC50 of six flavonoid compounds were 47–381 μM. Quercetin, epigallocatechin gallate and gallocatechin gallate (GCG) displayed good inhibition toward 3CLpro with IC50 values of 73, 73 and 47 μM, respectively. GCG showed a competitive inhibition pattern with Ki value of 25 ± 1.7 μM. In molecular docking experiments, GCG displayed a binding energy of −14 kcal mol−1 to the active site of 3CLpro and the galloyl moiety at 3-OH position was required for 3CLpro inhibition activity.Electronic supplementary materialThe online version of this article (doi:10.1007/s10529-011-0845-8) contains supplementary material, which is available to authorized users.

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Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris 원문보기

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Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris 원문보기

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