Identification of benzimidazole-based inhibitors of the mitogen activated kinase-5 signaling pathway
Identification of novel benzimidazole inhibitors of MEK5 mediated phosphorylation of ERK5 is presented and early effects of structure on activity are presented. The MEK-signaling pathways are complex but critical signaling cascades that correlate an extracellular signaling event with internal cell p...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-05, Vol.20 (9), p.2892-2896 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Flaherty, Patrick T. Chopra, Ishveen Jain, Prashi Yi, Shuyan Allen, Erika Cavanaugh, Jane |
| description | Identification of novel benzimidazole inhibitors of MEK5 mediated phosphorylation of ERK5 is presented and early effects of structure on activity are presented.
The MEK-signaling pathways are complex but critical signaling cascades that correlate an extracellular signaling event with internal cell processes. To date at least seven MEK isozymes have been identified. MEK5, in particular, is upregulated in multiple forms of tumors. Analysis of the EGF-induced MEK5 signaling cascade in cultured HEK cells has identified compounds that can inhibit MEK5 phosphorylation of ERK5; observed biological activity is dependent on chemical variation. |
| doi_str_mv | 10.1016/j.bmcl.2010.03.033 |
| format | Article |
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The MEK-signaling pathways are complex but critical signaling cascades that correlate an extracellular signaling event with internal cell processes. To date at least seven MEK isozymes have been identified. MEK5, in particular, is upregulated in multiple forms of tumors. Analysis of the EGF-induced MEK5 signaling cascade in cultured HEK cells has identified compounds that can inhibit MEK5 phosphorylation of ERK5; observed biological activity is dependent on chemical variation.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2010.03.033</identifier><identifier>PMID: 20382528</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Analytical, structural and metabolic biochemistry ; Benzimidazole ; Benzimidazoles - chemical synthesis ; Benzimidazoles - chemistry ; Benzimidazoles - pharmacology ; Biological and medical sciences ; Cell Line ; Enzymes and enzyme inhibitors ; Epidermal Growth Factor - pharmacology ; ERK5 ; Fundamental and applied biological sciences. Psychology ; Humans ; Inhibitor ; MAP Kinase Kinase 5 - antagonists & inhibitors ; MAP Kinase Kinase 5 - metabolism ; Medical sciences ; MEK5 ; Miscellaneous ; Mitogen-Activated Protein Kinase 7 - metabolism ; Pharmacology. Drug treatments ; Phosphorylation ; Protein Kinase Inhibitors - chemical synthesis ; Protein Kinase Inhibitors - chemistry ; Protein Kinase Inhibitors - pharmacology ; Signal Transduction - drug effects ; Transferases</subject><ispartof>Bioorganic & medicinal chemistry letters, 2010-05, Vol.20 (9), p.2892-2896</ispartof><rights>2010 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>2010 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c417t-1b0ae74299fc86a4dee202f8cf4def03c5a1cc2bf89a992c0e7548a72e62b2c3</citedby><cites>FETCH-LOGICAL-c417t-1b0ae74299fc86a4dee202f8cf4def03c5a1cc2bf89a992c0e7548a72e62b2c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2010.03.033$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,781,785,3551,27929,27930,46000</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22825029$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20382528$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Flaherty, Patrick T.</creatorcontrib><creatorcontrib>Chopra, Ishveen</creatorcontrib><creatorcontrib>Jain, Prashi</creatorcontrib><creatorcontrib>Yi, Shuyan</creatorcontrib><creatorcontrib>Allen, Erika</creatorcontrib><creatorcontrib>Cavanaugh, Jane</creatorcontrib><title>Identification of benzimidazole-based inhibitors of the mitogen activated kinase-5 signaling pathway</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Identification of novel benzimidazole inhibitors of MEK5 mediated phosphorylation of ERK5 is presented and early effects of structure on activity are presented.
The MEK-signaling pathways are complex but critical signaling cascades that correlate an extracellular signaling event with internal cell processes. To date at least seven MEK isozymes have been identified. MEK5, in particular, is upregulated in multiple forms of tumors. Analysis of the EGF-induced MEK5 signaling cascade in cultured HEK cells has identified compounds that can inhibit MEK5 phosphorylation of ERK5; observed biological activity is dependent on chemical variation.</description><subject>Analytical, structural and metabolic biochemistry</subject><subject>Benzimidazole</subject><subject>Benzimidazoles - chemical synthesis</subject><subject>Benzimidazoles - chemistry</subject><subject>Benzimidazoles - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Cell Line</subject><subject>Enzymes and enzyme inhibitors</subject><subject>Epidermal Growth Factor - pharmacology</subject><subject>ERK5</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Humans</subject><subject>Inhibitor</subject><subject>MAP Kinase Kinase 5 - antagonists & inhibitors</subject><subject>MAP Kinase Kinase 5 - metabolism</subject><subject>Medical sciences</subject><subject>MEK5</subject><subject>Miscellaneous</subject><subject>Mitogen-Activated Protein Kinase 7 - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Phosphorylation</subject><subject>Protein Kinase Inhibitors - chemical synthesis</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Protein Kinase Inhibitors - pharmacology</subject><subject>Signal Transduction - drug effects</subject><subject>Transferases</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0Utr3DAQAGBRWpptkj_QQ_Gl9OSNXn4Ieimhj0Aglxx6E2N5tDtbW95a2oTk11dmt-2thQE9-DQaZhh7K_hacFFf7dbd6Ia15PmCqxzqBVsJXetSaV69ZCtual62Rn8_Y29i3HEuNNf6NTuTXLWyku2K9Tc9hkSeHCSaQjH5osPwTCP18DwNWHYQsS8obKmjNM1xEWmLxZhPGwwFuEQPkLL5QSHbsioibQIMFDbFHtL2EZ4u2CsPQ8TL03rO7r98vr_-Vt7efb25_nRbOi2aVIqOAzZaGuNdW4PuESWXvnU-bz1XrgLhnOx8a8AY6Tg2lW6hkVjLTjp1zj4c0-7n6ecBY7IjRYfDAAGnQ7SNrmpjdKv-L5VqTZMLyVIepZunGGf0dj_TCPOTFdwuU7A7u0zBLlOwXOVY0r87pT90I_Z_nvxuewbvTwCig8HPEBzFv05mxuXy-8ejw9y1B8LZRkcYHPY0o0u2n-hfdfwCOYunRA</recordid><startdate>20100501</startdate><enddate>20100501</enddate><creator>Flaherty, Patrick T.</creator><creator>Chopra, Ishveen</creator><creator>Jain, Prashi</creator><creator>Yi, Shuyan</creator><creator>Allen, Erika</creator><creator>Cavanaugh, Jane</creator><general>Elsevier Ltd</general><general>Elsevier</general><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>7X8</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20100501</creationdate><title>Identification of benzimidazole-based inhibitors of the mitogen activated kinase-5 signaling pathway</title><author>Flaherty, Patrick T. ; Chopra, Ishveen ; Jain, Prashi ; Yi, Shuyan ; Allen, Erika ; Cavanaugh, Jane</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c417t-1b0ae74299fc86a4dee202f8cf4def03c5a1cc2bf89a992c0e7548a72e62b2c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Analytical, structural and metabolic biochemistry</topic><topic>Benzimidazole</topic><topic>Benzimidazoles - chemical synthesis</topic><topic>Benzimidazoles - chemistry</topic><topic>Benzimidazoles - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Cell Line</topic><topic>Enzymes and enzyme inhibitors</topic><topic>Epidermal Growth Factor - pharmacology</topic><topic>ERK5</topic><topic>Fundamental and applied biological sciences. 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Drug treatments</topic><topic>Phosphorylation</topic><topic>Protein Kinase Inhibitors - chemical synthesis</topic><topic>Protein Kinase Inhibitors - chemistry</topic><topic>Protein Kinase Inhibitors - pharmacology</topic><topic>Signal Transduction - drug effects</topic><topic>Transferases</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Flaherty, Patrick T.</creatorcontrib><creatorcontrib>Chopra, Ishveen</creatorcontrib><creatorcontrib>Jain, Prashi</creatorcontrib><creatorcontrib>Yi, Shuyan</creatorcontrib><creatorcontrib>Allen, Erika</creatorcontrib><creatorcontrib>Cavanaugh, Jane</creatorcontrib><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>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Flaherty, Patrick T.</au><au>Chopra, Ishveen</au><au>Jain, Prashi</au><au>Yi, Shuyan</au><au>Allen, Erika</au><au>Cavanaugh, Jane</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Identification of benzimidazole-based inhibitors of the mitogen activated kinase-5 signaling pathway</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2010-05-01</date><risdate>2010</risdate><volume>20</volume><issue>9</issue><spage>2892</spage><epage>2896</epage><pages>2892-2896</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Identification of novel benzimidazole inhibitors of MEK5 mediated phosphorylation of ERK5 is presented and early effects of structure on activity are presented.
The MEK-signaling pathways are complex but critical signaling cascades that correlate an extracellular signaling event with internal cell processes. To date at least seven MEK isozymes have been identified. MEK5, in particular, is upregulated in multiple forms of tumors. Analysis of the EGF-induced MEK5 signaling cascade in cultured HEK cells has identified compounds that can inhibit MEK5 phosphorylation of ERK5; observed biological activity is dependent on chemical variation.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>20382528</pmid><doi>10.1016/j.bmcl.2010.03.033</doi><tpages>5</tpages></addata></record> |
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| subjects | Analytical, structural and metabolic biochemistry Benzimidazole Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Cell Line Enzymes and enzyme inhibitors Epidermal Growth Factor - pharmacology ERK5 Fundamental and applied biological sciences. Psychology Humans Inhibitor MAP Kinase Kinase 5 - antagonists & inhibitors MAP Kinase Kinase 5 - metabolism Medical sciences MEK5 Miscellaneous Mitogen-Activated Protein Kinase 7 - metabolism Pharmacology. Drug treatments Phosphorylation Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Signal Transduction - drug effects Transferases |
| title | Identification of benzimidazole-based inhibitors of the mitogen activated kinase-5 signaling pathway |
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