Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT)
[Display omitted] Inhibition of soluble epoxide hydrolase (sEH) has recently emerged as a new approach to treat cardiovascular disease and respiratory disease. Inhibitors based on 1,3,5-triazine chemotype were discovered through affinity selection against two triazine-based DNA-encoded libraries. Th...
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Veröffentlicht in: | Bioorganic & medicinal chemistry 2021-07, Vol.41, p.116216-116216, Article 116216 |
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container_title | Bioorganic & medicinal chemistry |
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creator | Ding, Yun Belyanskaya, Svetlana DeLorey, Jennifer L. Messer, Jeffrey A. Joseph Franklin, G. Centrella, Paolo A. Morgan, Barry A. Clark, Matthew A. Skinner, Steven R. Dodson, Jason W. Li, Peng Marino, Joseph P. Israel, David I. |
description | [Display omitted]
Inhibition of soluble epoxide hydrolase (sEH) has recently emerged as a new approach to treat cardiovascular disease and respiratory disease. Inhibitors based on 1,3,5-triazine chemotype were discovered through affinity selection against two triazine-based DNA-encoded libraries. The structure and activity relationship study led to the expansion of the original 1,4-cycloalkyl series to related aniline, piperidine, quinoline, aryl-ether and benzylic series. The 1,3-cycloalkyl chemotype led to the discovery of a clinical candidate (GSK2256294) for COPD. |
doi_str_mv | 10.1016/j.bmc.2021.116216 |
format | Article |
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Inhibition of soluble epoxide hydrolase (sEH) has recently emerged as a new approach to treat cardiovascular disease and respiratory disease. Inhibitors based on 1,3,5-triazine chemotype were discovered through affinity selection against two triazine-based DNA-encoded libraries. The structure and activity relationship study led to the expansion of the original 1,4-cycloalkyl series to related aniline, piperidine, quinoline, aryl-ether and benzylic series. The 1,3-cycloalkyl chemotype led to the discovery of a clinical candidate (GSK2256294) for COPD.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2021.116216</identifier><language>eng</language><publisher>Elsevier Ltd</publisher><subject>DNA-encoded library technology ; Soluble epoxide hydrolase</subject><ispartof>Bioorganic & medicinal chemistry, 2021-07, Vol.41, p.116216-116216, Article 116216</ispartof><rights>2021 Elsevier Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c330t-e3c3cd138b47db7b03f24e4198f4e1d22dcda4ef728c0f3b18f3073accbce3e53</citedby><cites>FETCH-LOGICAL-c330t-e3c3cd138b47db7b03f24e4198f4e1d22dcda4ef728c0f3b18f3073accbce3e53</cites><orcidid>0000-0002-9650-9332 ; 0000-0002-3809-6170</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0968089621002248$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65534</link.rule.ids></links><search><creatorcontrib>Ding, Yun</creatorcontrib><creatorcontrib>Belyanskaya, Svetlana</creatorcontrib><creatorcontrib>DeLorey, Jennifer L.</creatorcontrib><creatorcontrib>Messer, Jeffrey A.</creatorcontrib><creatorcontrib>Joseph Franklin, G.</creatorcontrib><creatorcontrib>Centrella, Paolo A.</creatorcontrib><creatorcontrib>Morgan, Barry A.</creatorcontrib><creatorcontrib>Clark, Matthew A.</creatorcontrib><creatorcontrib>Skinner, Steven R.</creatorcontrib><creatorcontrib>Dodson, Jason W.</creatorcontrib><creatorcontrib>Li, Peng</creatorcontrib><creatorcontrib>Marino, Joseph P.</creatorcontrib><creatorcontrib>Israel, David I.</creatorcontrib><title>Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT)</title><title>Bioorganic & medicinal chemistry</title><description>[Display omitted]
Inhibition of soluble epoxide hydrolase (sEH) has recently emerged as a new approach to treat cardiovascular disease and respiratory disease. Inhibitors based on 1,3,5-triazine chemotype were discovered through affinity selection against two triazine-based DNA-encoded libraries. The structure and activity relationship study led to the expansion of the original 1,4-cycloalkyl series to related aniline, piperidine, quinoline, aryl-ether and benzylic series. The 1,3-cycloalkyl chemotype led to the discovery of a clinical candidate (GSK2256294) for COPD.</description><subject>DNA-encoded library technology</subject><subject>Soluble epoxide hydrolase</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNp9kEtPAjEUhRujiYj-AHdd4mKwty3ziCsC-EiIbnBrM23vMCXDFNuByL93CK5d3c05J_f7CLkHNgYG6eNmrLdmzBmHMUDKIb0gA5CpTIQo4JIMWJHmCcuL9JrcxLhhjHFZwIB8zV00_oDhSH1Fo2_2ukGKO__jLNL6aINvyojUtbXTrvMh0q4Ofr-u6fx9mmBrvEVLG6dD2W90aOrWN359pKPFcvVwS66qsol493eH5PN5sZq9JsuPl7fZdJkYIViXoDDCWBC5lpnVmWai4hIlFHklESzn1thSYpXx3LBKaMgrwTJRGqMNCpyIIRmdd3fBf-8xdmrbc2HTlC36fVR8ImAiRc7yPgrnqAk-xoCV2gW37Z9XwNTJpdqo3qU6uVRnl33n6dzBnuHgMKhoXM-O1gU0nbLe_dP-BSI-fX4</recordid><startdate>20210701</startdate><enddate>20210701</enddate><creator>Ding, Yun</creator><creator>Belyanskaya, Svetlana</creator><creator>DeLorey, Jennifer L.</creator><creator>Messer, Jeffrey A.</creator><creator>Joseph Franklin, G.</creator><creator>Centrella, Paolo A.</creator><creator>Morgan, Barry A.</creator><creator>Clark, Matthew A.</creator><creator>Skinner, Steven R.</creator><creator>Dodson, Jason W.</creator><creator>Li, Peng</creator><creator>Marino, Joseph P.</creator><creator>Israel, David I.</creator><general>Elsevier Ltd</general><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0002-9650-9332</orcidid><orcidid>https://orcid.org/0000-0002-3809-6170</orcidid></search><sort><creationdate>20210701</creationdate><title>Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT)</title><author>Ding, Yun ; Belyanskaya, Svetlana ; DeLorey, Jennifer L. ; Messer, Jeffrey A. ; Joseph Franklin, G. ; Centrella, Paolo A. ; Morgan, Barry A. ; Clark, Matthew A. ; Skinner, Steven R. ; Dodson, Jason W. ; Li, Peng ; Marino, Joseph P. ; Israel, David I.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c330t-e3c3cd138b47db7b03f24e4198f4e1d22dcda4ef728c0f3b18f3073accbce3e53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>DNA-encoded library technology</topic><topic>Soluble epoxide hydrolase</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ding, Yun</creatorcontrib><creatorcontrib>Belyanskaya, Svetlana</creatorcontrib><creatorcontrib>DeLorey, Jennifer L.</creatorcontrib><creatorcontrib>Messer, Jeffrey A.</creatorcontrib><creatorcontrib>Joseph Franklin, G.</creatorcontrib><creatorcontrib>Centrella, Paolo A.</creatorcontrib><creatorcontrib>Morgan, Barry A.</creatorcontrib><creatorcontrib>Clark, Matthew A.</creatorcontrib><creatorcontrib>Skinner, Steven R.</creatorcontrib><creatorcontrib>Dodson, Jason W.</creatorcontrib><creatorcontrib>Li, Peng</creatorcontrib><creatorcontrib>Marino, Joseph P.</creatorcontrib><creatorcontrib>Israel, David I.</creatorcontrib><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ding, Yun</au><au>Belyanskaya, Svetlana</au><au>DeLorey, Jennifer L.</au><au>Messer, Jeffrey A.</au><au>Joseph Franklin, G.</au><au>Centrella, Paolo A.</au><au>Morgan, Barry A.</au><au>Clark, Matthew A.</au><au>Skinner, Steven R.</au><au>Dodson, Jason W.</au><au>Li, Peng</au><au>Marino, Joseph P.</au><au>Israel, David I.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT)</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><date>2021-07-01</date><risdate>2021</risdate><volume>41</volume><spage>116216</spage><epage>116216</epage><pages>116216-116216</pages><artnum>116216</artnum><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>[Display omitted]
Inhibition of soluble epoxide hydrolase (sEH) has recently emerged as a new approach to treat cardiovascular disease and respiratory disease. Inhibitors based on 1,3,5-triazine chemotype were discovered through affinity selection against two triazine-based DNA-encoded libraries. The structure and activity relationship study led to the expansion of the original 1,4-cycloalkyl series to related aniline, piperidine, quinoline, aryl-ether and benzylic series. The 1,3-cycloalkyl chemotype led to the discovery of a clinical candidate (GSK2256294) for COPD.</abstract><pub>Elsevier Ltd</pub><doi>10.1016/j.bmc.2021.116216</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0002-9650-9332</orcidid><orcidid>https://orcid.org/0000-0002-3809-6170</orcidid></addata></record> |
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subjects | DNA-encoded library technology Soluble epoxide hydrolase |
title | Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT) |
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