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- Title
Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris.
- Authors
Nguyen, Thi; Woo, Hye-Jin; Kang, Hee-Kyoung; Nguyen, Van; Kim, Young-Min; Kim, Do-Won; Ahn, Sul-Ah; Xia, Yongmei; Kim, Doman
- Abstract
The 3C-like protease (3CL) of severe acute respiratory syndrome associated coronavirus (SARS-CoV) is vital for SARS-CoV replication and is a promising drug target. Recombinant 3CL was expressed in Pichia pastoris GS115 as a 42 kDa protein that displayed a K of 15 ± 2 μM with Dabcyl-KTSAVLQSGFRKME-Edans as substrate. Purified 3CL was used for inhibition and kinetic assays with seven flavonoid compounds. The IC of six flavonoid compounds were 47-381 μM. Quercetin, epigallocatechin gallate and gallocatechin gallate (GCG) displayed good inhibition toward 3CL with IC values of 73, 73 and 47 μM, respectively. GCG showed a competitive inhibition pattern with K value of 25 ± 1.7 μM. In molecular docking experiments, GCG displayed a binding energy of −14 kcal mol to the active site of 3CL and the galloyl moiety at 3-OH position was required for 3CL inhibition activity.
- Subjects
FLAVONOIDS; SARS disease; PICHIA pastoris; RECOMBINANT protease inhibitors; PROTEOLYTIC enzymes
- Publication
Biotechnology Letters, 2012, Vol 34, Issue 5, p831
- ISSN
0141-5492
- Publication type
Article
- DOI
10.1007/s10529-011-0845-8