Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris = 플라보노이드 유래 SARS coronavirus 3CL protease 저해 특성

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Title
Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris = 플라보노이드 유래 SARS coronavirus 3CL protease 저해 특성
Author(s)
T T H Nguyen; H J Woo; H K Kang; V D Nguyen; Young Min Kim; D W Kim; S A Ahn; Y Xia; D Kim
Bibliographic Citation
Biotechnology Letters, vol. 34, no. 5, pp. 831-838
Publication Year
2012
Abstract
The 3C-like protease (3CL pro) of severe acute respiratory syndrome associated coronavirus (SARS-CoV) is vital for SARS-CoV replication and is a promising drug target. Recombinant 3CL pro was expressed in Pichia pastoris GS115 as a 42 kDa protein that displayed a K m of 15 ± 2 μM with Dabcyl-KTSAVLQSGFRKME-Edans as substrate. Purified 3CL pro was used for inhibition and kinetic assays with seven flavonoid compounds. The IC 50 of six flavonoidcompounds were 47-381 μM. Quercetin, epigallocatechin gallate and gallocatechin gallate (GCG) displayed good inhibition toward 3CL pro with IC 50 values of 73, 73 and 47 μM, respectively. GCG showed a competitive inhibition pattern with K i 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 3CL pro and the galloyl moiety at 3-OH position was required for 3CL pro inhibition activity.
Keyword
FlavonoidMolecular dockingPichia pastorisProteaseSevere acute respiratory syndrome (SARS)
ISSN
0141-5492
Publisher
Springer
DOI
http://dx.doi.org/10.1007/s10529-011-0845-8
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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