Erkitinib, a novel EGFR tyrosine kinase inhibitor screened using a ProteoChip system from a phytochemical library
Receptor tyrosine kinases (PTKs) play key roles in the pathogenesis of numerous human diseases, including cancer. Therefore PTK inhibitors are currently under intensive investigation as potential drug candidates. Herein, we report on a ProteoChip-based screening of an epidermal growth factor recepto...
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| Veröffentlicht in: | Biochemical and biophysical research communications 2009-11, Vol.389 (3), p.415-419 |
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| container_title | Biochemical and biophysical research communications |
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| creator | Kim, Eung-Yoon Choi, Young-Jin Park, Chan-Won Kang, In-Cheol |
| description | Receptor tyrosine kinases (PTKs) play key roles in the pathogenesis of numerous human diseases, including cancer. Therefore PTK inhibitors are currently under intensive investigation as potential drug candidates. Herein, we report on a ProteoChip-based screening of an epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitor, Erkitinibs, from phytochemical libraries. PLC-γ-1 was used as a substrate immobilized on a ProteoChip and incubated with an EGFR kinase to phosphorylate tyrosine residues of the substrate, followed by a fluorescence detection of the substrate recognized by a phospho-specific monoclonal antibody. Erkitinibs inhibited HeLa cell proliferation in a dose-dependent manner. In conclusion, these data suggest that Erkitinibs can be a specific inhibitor of an EGFR kinase and can be further developed as a potent anti-tumor agent. |
| doi_str_mv | 10.1016/j.bbrc.2009.08.141 |
| format | Article |
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Therefore PTK inhibitors are currently under intensive investigation as potential drug candidates. Herein, we report on a ProteoChip-based screening of an epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitor, Erkitinibs, from phytochemical libraries. PLC-γ-1 was used as a substrate immobilized on a ProteoChip and incubated with an EGFR kinase to phosphorylate tyrosine residues of the substrate, followed by a fluorescence detection of the substrate recognized by a phospho-specific monoclonal antibody. Erkitinibs inhibited HeLa cell proliferation in a dose-dependent manner. In conclusion, these data suggest that Erkitinibs can be a specific inhibitor of an EGFR kinase and can be further developed as a potent anti-tumor agent.</description><subject>60 APPLIED LIFE SCIENCES</subject><subject>Anti-tumor agent</subject><subject>Antineoplastic Agents, Phytogenic - chemistry</subject><subject>Antineoplastic Agents, Phytogenic - isolation & purification</subject><subject>Antineoplastic Agents, Phytogenic - pharmacology</subject><subject>Drug Screening Assays, Antitumor</subject><subject>EGFR kinase</subject><subject>EGFR kinase inhibitor</subject><subject>FLUORESCENCE</subject><subject>GROWTH FACTORS</subject><subject>HELA CELLS</subject><subject>Humans</subject><subject>In silico virtual screening</subject><subject>MONOCLONAL ANTIBODIES</subject><subject>NEOPLASMS</subject><subject>PHOSPHOTRANSFERASES</subject><subject>Protein Array Analysis - methods</subject><subject>Protein chip</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Protein Kinase Inhibitors - isolation & purification</subject><subject>Protein Kinase Inhibitors - pharmacology</subject><subject>Receptor, Epidermal Growth Factor - antagonists & inhibitors</subject><subject>RECEPTORS</subject><subject>SCREENING</subject><subject>SUBSTRATES</subject><subject>TYROSINE</subject><issn>0006-291X</issn><issn>1090-2104</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kUGLFDEQhYMo7rj6BzxIQPBkj6l0T3cCXpZhdhUWFFHwFpJ0tZ3Z7mQ2ySzMvzfNDHjzVIf63qPqPULeAlsDg_bTfm1MtGvOmFwzsYYGnpEVMMkqDqx5TlaMsbbiEn5fkVcp7RkDaFr5klyB7KAVrFmRx118cNl5Zz5STX14wonu7m5_0HyKITmP9MF5nZA6Pzrjcog02YjosafHsv9TVN9jyBi2ozvQdEoZZzrEMJfFYTzlYEecndUTnZyJOp5ekxeDnhK-ucxr8ut293P7pbr_dvd1e3Nf2VrwXIFtNHRQS6F5owfZ8FowY4UxBuUw1ANvbNfLjTRa1IigB2w2KOvBgjEbvamvyfuzb0jZqWRdRjva4D3arDgHKUXXFerDmTrE8HjElNXsksVp0h7DMam2a4WAti4gP4O25JIiDuoQ3Vz-UcDUUofaq6UOtdShmFCljiJ6d3E_mhn7f5JL_gX4fAawJPHkMC6HorfYu7jc2Qf3P_-_LiydQw</recordid><startdate>20091120</startdate><enddate>20091120</enddate><creator>Kim, Eung-Yoon</creator><creator>Choi, Young-Jin</creator><creator>Park, Chan-Won</creator><creator>Kang, In-Cheol</creator><general>Elsevier Inc</general><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>7X8</scope><scope>OTOTI</scope></search><sort><creationdate>20091120</creationdate><title>Erkitinib, a novel EGFR tyrosine kinase inhibitor screened using a ProteoChip system from a phytochemical library</title><author>Kim, Eung-Yoon ; Choi, Young-Jin ; Park, Chan-Won ; Kang, In-Cheol</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c382t-1c4a171398a24af942380bc8bbbe9ff3f24c7d959ba83ee1afe45e93fc1bb5a53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>60 APPLIED LIFE SCIENCES</topic><topic>Anti-tumor agent</topic><topic>Antineoplastic Agents, Phytogenic - chemistry</topic><topic>Antineoplastic Agents, Phytogenic - isolation & purification</topic><topic>Antineoplastic Agents, Phytogenic - pharmacology</topic><topic>Drug Screening Assays, Antitumor</topic><topic>EGFR kinase</topic><topic>EGFR kinase inhibitor</topic><topic>FLUORESCENCE</topic><topic>GROWTH FACTORS</topic><topic>HELA CELLS</topic><topic>Humans</topic><topic>In silico virtual screening</topic><topic>MONOCLONAL ANTIBODIES</topic><topic>NEOPLASMS</topic><topic>PHOSPHOTRANSFERASES</topic><topic>Protein Array Analysis - methods</topic><topic>Protein chip</topic><topic>Protein Kinase Inhibitors - chemistry</topic><topic>Protein Kinase Inhibitors - isolation & purification</topic><topic>Protein Kinase Inhibitors - pharmacology</topic><topic>Receptor, Epidermal Growth Factor - antagonists & inhibitors</topic><topic>RECEPTORS</topic><topic>SCREENING</topic><topic>SUBSTRATES</topic><topic>TYROSINE</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kim, Eung-Yoon</creatorcontrib><creatorcontrib>Choi, Young-Jin</creatorcontrib><creatorcontrib>Park, Chan-Won</creatorcontrib><creatorcontrib>Kang, In-Cheol</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>OSTI.GOV</collection><jtitle>Biochemical and biophysical research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kim, Eung-Yoon</au><au>Choi, Young-Jin</au><au>Park, Chan-Won</au><au>Kang, In-Cheol</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Erkitinib, a novel EGFR tyrosine kinase inhibitor screened using a ProteoChip system from a phytochemical library</atitle><jtitle>Biochemical and biophysical research communications</jtitle><addtitle>Biochem Biophys Res Commun</addtitle><date>2009-11-20</date><risdate>2009</risdate><volume>389</volume><issue>3</issue><spage>415</spage><epage>419</epage><pages>415-419</pages><issn>0006-291X</issn><eissn>1090-2104</eissn><abstract>Receptor tyrosine kinases (PTKs) play key roles in the pathogenesis of numerous human diseases, including cancer. Therefore PTK inhibitors are currently under intensive investigation as potential drug candidates. Herein, we report on a ProteoChip-based screening of an epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitor, Erkitinibs, from phytochemical libraries. PLC-γ-1 was used as a substrate immobilized on a ProteoChip and incubated with an EGFR kinase to phosphorylate tyrosine residues of the substrate, followed by a fluorescence detection of the substrate recognized by a phospho-specific monoclonal antibody. Erkitinibs inhibited HeLa cell proliferation in a dose-dependent manner. In conclusion, these data suggest that Erkitinibs can be a specific inhibitor of an EGFR kinase and can be further developed as a potent anti-tumor agent.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>19716804</pmid><doi>10.1016/j.bbrc.2009.08.141</doi><tpages>5</tpages></addata></record> |
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| subjects | 60 APPLIED LIFE SCIENCES Anti-tumor agent Antineoplastic Agents, Phytogenic - chemistry Antineoplastic Agents, Phytogenic - isolation & purification Antineoplastic Agents, Phytogenic - pharmacology Drug Screening Assays, Antitumor EGFR kinase EGFR kinase inhibitor FLUORESCENCE GROWTH FACTORS HELA CELLS Humans In silico virtual screening MONOCLONAL ANTIBODIES NEOPLASMS PHOSPHOTRANSFERASES Protein Array Analysis - methods Protein chip Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - isolation & purification Protein Kinase Inhibitors - pharmacology Receptor, Epidermal Growth Factor - antagonists & inhibitors RECEPTORS SCREENING SUBSTRATES TYROSINE |
| title | Erkitinib, a novel EGFR tyrosine kinase inhibitor screened using a ProteoChip system from a phytochemical library |
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