Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris
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 K m of 15 ± 2 μM with Dabcyl-KTSAVLQSG...
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| Veröffentlicht in: | Biotechnology letters 2012-05, Vol.34 (5), p.831-838 |
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| creator | 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 |
| description | 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 K m 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 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 3CLpro and the galloyl moiety at 3-OH position was required for 3CLpro inhibition activity. |
| doi_str_mv | 10.1007/s10529-011-0845-8 |
| format | Article |
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Recombinant 3CLpro 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 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 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 3CLpro and the galloyl moiety at 3-OH position was required for 3CLpro inhibition activity.</description><identifier>ISSN: 0141-5492</identifier><identifier>EISSN: 1573-6776</identifier><identifier>DOI: 10.1007/s10529-011-0845-8</identifier><identifier>PMID: 22350287</identifier><identifier>CODEN: BILED3</identifier><language>eng</language><publisher>Dordrecht: Springer-Verlag</publisher><subject>Applied Microbiology ; Biochemistry ; Biological and medical sciences ; Biomedical and Life Sciences ; Biotechnology ; Catechin - analogs & derivatives ; Catechin - metabolism ; Cysteine Endopeptidases - biosynthesis ; Cysteine Endopeptidases - chemistry ; Cysteine Endopeptidases - genetics ; drugs ; energy ; epigallocatechin ; Flavonoids ; Flavonoids - metabolism ; Fundamental and applied biological sciences. Psychology ; Gallates ; Gene Expression ; Hydrolysis ; Inhibition ; Inhibitory Concentration 50 ; Kinetics ; Life Sciences ; Microbiology ; Molecular Weight ; Original Research Paper ; Pichia - genetics ; Pichia pastoris ; Protease ; Protease Inhibitors - metabolism ; Proteases ; proteinases ; quercetin ; Recombinant ; Recombinant Proteins - antagonists & inhibitors ; Recombinant Proteins - biosynthesis ; Recombinant Proteins - chemistry ; Recombinant Proteins - genetics ; SARS coronavirus ; SARS Virus - enzymology ; SARS Virus - genetics ; Severe Acute Respiratory Syndrome ; Viral Proteins - antagonists & inhibitors ; Viral Proteins - biosynthesis ; Viral Proteins - chemistry ; Viral Proteins - genetics</subject><ispartof>Biotechnology letters, 2012-05, Vol.34 (5), p.831-838</ispartof><rights>Springer Science+Business Media B.V. 2012</rights><rights>2015 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c656t-31016bcdc82c1c7dfed4e951d7007ee81cad967dfdf972f1d0d224a9d3c4f82d3</citedby><cites>FETCH-LOGICAL-c656t-31016bcdc82c1c7dfed4e951d7007ee81cad967dfdf972f1d0d224a9d3c4f82d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s10529-011-0845-8$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s10529-011-0845-8$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>230,314,776,780,881,27901,27902,41464,42533,51294</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=25812388$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22350287$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Nguyen, Thi Thanh Hanh</creatorcontrib><creatorcontrib>Woo, Hye-Jin</creatorcontrib><creatorcontrib>Kang, Hee-Kyoung</creatorcontrib><creatorcontrib>Nguyen, Van Dao</creatorcontrib><creatorcontrib>Kim, Young-Min</creatorcontrib><creatorcontrib>Kim, Do-Won</creatorcontrib><creatorcontrib>Ahn, Sul-Ah</creatorcontrib><creatorcontrib>Xia, Yongmei</creatorcontrib><creatorcontrib>Kim, Doman</creatorcontrib><title>Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris</title><title>Biotechnology letters</title><addtitle>Biotechnol Lett</addtitle><addtitle>Biotechnol Lett</addtitle><description>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 K m 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 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 3CLpro and the galloyl moiety at 3-OH position was required for 3CLpro inhibition activity.</description><subject>Applied Microbiology</subject><subject>Biochemistry</subject><subject>Biological and medical sciences</subject><subject>Biomedical and Life Sciences</subject><subject>Biotechnology</subject><subject>Catechin - analogs & derivatives</subject><subject>Catechin - metabolism</subject><subject>Cysteine Endopeptidases - biosynthesis</subject><subject>Cysteine Endopeptidases - chemistry</subject><subject>Cysteine Endopeptidases - genetics</subject><subject>drugs</subject><subject>energy</subject><subject>epigallocatechin</subject><subject>Flavonoids</subject><subject>Flavonoids - metabolism</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Gallates</subject><subject>Gene Expression</subject><subject>Hydrolysis</subject><subject>Inhibition</subject><subject>Inhibitory Concentration 50</subject><subject>Kinetics</subject><subject>Life Sciences</subject><subject>Microbiology</subject><subject>Molecular Weight</subject><subject>Original Research Paper</subject><subject>Pichia - genetics</subject><subject>Pichia pastoris</subject><subject>Protease</subject><subject>Protease Inhibitors - metabolism</subject><subject>Proteases</subject><subject>proteinases</subject><subject>quercetin</subject><subject>Recombinant</subject><subject>Recombinant Proteins - antagonists & inhibitors</subject><subject>Recombinant Proteins - biosynthesis</subject><subject>Recombinant Proteins - chemistry</subject><subject>Recombinant Proteins - genetics</subject><subject>SARS coronavirus</subject><subject>SARS Virus - enzymology</subject><subject>SARS Virus - genetics</subject><subject>Severe Acute Respiratory Syndrome</subject><subject>Viral Proteins - antagonists & inhibitors</subject><subject>Viral Proteins - biosynthesis</subject><subject>Viral Proteins - chemistry</subject><subject>Viral Proteins - genetics</subject><issn>0141-5492</issn><issn>1573-6776</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><recordid>eNqFkl9rFDEUxQdR7Lb6AXzRASn4Es1NJn_mRSiLVaGguPY5ZJPMbupssiYzi357M85aqyA-BZLfPfeenFtVTwC_BIzFqwyYkRZhAIRlw5C8Vy2ACYq4EPx-tcDQAGJNS06q05xvMMatwOJhdUIIZZhIsajUZa8PMURv0c5Zrwdnax-2fu0HH0Mdu3p18WlVm5hi0AefxlzTJer9F1fvUxyczq523_bJ5fyzsv7ozdbreq_zEJPPj6oHne6ze3w8z6rryzefl-_Q1Ye375cXV8hwxgdEAQNfG2skMWCE7ZxtXMvAiuLTOQlG25aXe9u1gnRgsSWk0a2lpukksfSsej3r7sd1MWJcGJLu1T75nU7fVdRe_fkS_FZt4kEJLAWTtAi8OAqk-HV0eVA7n43rex1cHLMCLpkEzqn8P4pBtBKA8II-_wu9iWMK5ScminIgkk-9YaZMijkn193ODVhNSas5aVWSVlPSahri6V3DtxW_oi3A-RHQ2ei-SzoYn39zxQ2hchIiM5fLU9i4dHfEf3d_Nhd1Oiq9KUGr6xUp-1Z2rOGYAf0BmjPKuw</recordid><startdate>20120501</startdate><enddate>20120501</enddate><creator>Nguyen, Thi Thanh Hanh</creator><creator>Woo, Hye-Jin</creator><creator>Kang, Hee-Kyoung</creator><creator>Nguyen, Van Dao</creator><creator>Kim, Young-Min</creator><creator>Kim, Do-Won</creator><creator>Ahn, Sul-Ah</creator><creator>Xia, Yongmei</creator><creator>Kim, Doman</creator><general>Springer-Verlag</general><general>Springer Netherlands</general><general>Springer</general><general>Springer Nature B.V</general><scope>FBQ</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7QL</scope><scope>7QR</scope><scope>7T7</scope><scope>7TB</scope><scope>7U5</scope><scope>7X7</scope><scope>7XB</scope><scope>88A</scope><scope>88E</scope><scope>88I</scope><scope>8AO</scope><scope>8FD</scope><scope>8FE</scope><scope>8FG</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABJCF</scope><scope>ABUWG</scope><scope>AEUYN</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>BHPHI</scope><scope>C1K</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>L6V</scope><scope>L7M</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M2P</scope><scope>M7N</scope><scope>M7P</scope><scope>M7S</scope><scope>P64</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PTHSS</scope><scope>Q9U</scope><scope>7QO</scope><scope>7U9</scope><scope>H94</scope><scope>5PM</scope></search><sort><creationdate>20120501</creationdate><title>Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris</title><author>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</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c656t-31016bcdc82c1c7dfed4e951d7007ee81cad967dfdf972f1d0d224a9d3c4f82d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Applied Microbiology</topic><topic>Biochemistry</topic><topic>Biological and medical sciences</topic><topic>Biomedical and Life Sciences</topic><topic>Biotechnology</topic><topic>Catechin - analogs & derivatives</topic><topic>Catechin - metabolism</topic><topic>Cysteine Endopeptidases - biosynthesis</topic><topic>Cysteine Endopeptidases - chemistry</topic><topic>Cysteine Endopeptidases - genetics</topic><topic>drugs</topic><topic>energy</topic><topic>epigallocatechin</topic><topic>Flavonoids</topic><topic>Flavonoids - metabolism</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Gallates</topic><topic>Gene Expression</topic><topic>Hydrolysis</topic><topic>Inhibition</topic><topic>Inhibitory Concentration 50</topic><topic>Kinetics</topic><topic>Life Sciences</topic><topic>Microbiology</topic><topic>Molecular Weight</topic><topic>Original Research Paper</topic><topic>Pichia - genetics</topic><topic>Pichia pastoris</topic><topic>Protease</topic><topic>Protease Inhibitors - metabolism</topic><topic>Proteases</topic><topic>proteinases</topic><topic>quercetin</topic><topic>Recombinant</topic><topic>Recombinant Proteins - antagonists & inhibitors</topic><topic>Recombinant Proteins - biosynthesis</topic><topic>Recombinant Proteins - chemistry</topic><topic>Recombinant Proteins - genetics</topic><topic>SARS coronavirus</topic><topic>SARS Virus - enzymology</topic><topic>SARS Virus - genetics</topic><topic>Severe Acute Respiratory Syndrome</topic><topic>Viral Proteins - antagonists & inhibitors</topic><topic>Viral Proteins - biosynthesis</topic><topic>Viral Proteins - chemistry</topic><topic>Viral Proteins - genetics</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nguyen, Thi Thanh Hanh</creatorcontrib><creatorcontrib>Woo, Hye-Jin</creatorcontrib><creatorcontrib>Kang, Hee-Kyoung</creatorcontrib><creatorcontrib>Nguyen, Van Dao</creatorcontrib><creatorcontrib>Kim, Young-Min</creatorcontrib><creatorcontrib>Kim, Do-Won</creatorcontrib><creatorcontrib>Ahn, Sul-Ah</creatorcontrib><creatorcontrib>Xia, Yongmei</creatorcontrib><creatorcontrib>Kim, Doman</creatorcontrib><collection>AGRIS</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Bacteriology Abstracts (Microbiology 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Lett</addtitle><date>2012-05-01</date><risdate>2012</risdate><volume>34</volume><issue>5</issue><spage>831</spage><epage>838</epage><pages>831-838</pages><issn>0141-5492</issn><eissn>1573-6776</eissn><coden>BILED3</coden><abstract>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 K m 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 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 3CLpro and the galloyl moiety at 3-OH position was required for 3CLpro inhibition activity.</abstract><cop>Dordrecht</cop><pub>Springer-Verlag</pub><pmid>22350287</pmid><doi>10.1007/s10529-011-0845-8</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Biotechnology letters, 2012-05, Vol.34 (5), p.831-838 |
| issn | 0141-5492 1573-6776 |
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| source | MEDLINE; Springer Nature - Complete Springer Journals |
| subjects | Applied Microbiology Biochemistry Biological and medical sciences Biomedical and Life Sciences Biotechnology Catechin - analogs & derivatives Catechin - metabolism Cysteine Endopeptidases - biosynthesis Cysteine Endopeptidases - chemistry Cysteine Endopeptidases - genetics drugs energy epigallocatechin Flavonoids Flavonoids - metabolism Fundamental and applied biological sciences. Psychology Gallates Gene Expression Hydrolysis Inhibition Inhibitory Concentration 50 Kinetics Life Sciences Microbiology Molecular Weight Original Research Paper Pichia - genetics Pichia pastoris Protease Protease Inhibitors - metabolism Proteases proteinases quercetin Recombinant Recombinant Proteins - antagonists & inhibitors Recombinant Proteins - biosynthesis Recombinant Proteins - chemistry Recombinant Proteins - genetics SARS coronavirus SARS Virus - enzymology SARS Virus - genetics Severe Acute Respiratory Syndrome Viral Proteins - antagonists & inhibitors Viral Proteins - biosynthesis Viral Proteins - chemistry Viral Proteins - genetics |
| title | Flavonoid-mediated inhibition of SARS coronavirus 3C-like protease expressed in Pichia pastoris |
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