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Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway
[Display omitted] Nrf2 is the major transcription factor that regulates many of the cytoprotective enzymes involved in the adaptive stress response. Modulation of Nrf2 could be therapeutically useful in a number of disease states. Activation can occur through either an electrophilic or non-electroph...
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| Published in: | Bioorganic & medicinal chemistry letters 2015-06, Vol.25 (11), p.2261-2268 |
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| Main Authors: | , , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c591t-cfad3895d8ff62204bd9eac13bd1778f016c1d106e34626ff88567fedddee5e03 |
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| cites | cdi_FETCH-LOGICAL-c591t-cfad3895d8ff62204bd9eac13bd1778f016c1d106e34626ff88567fedddee5e03 |
| container_end_page | 2268 |
| container_issue | 11 |
| container_start_page | 2261 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 25 |
| creator | Richardson, B.G. Jain, A.D. Speltz, T.E. Moore, T.W. |
| description | [Display omitted]
Nrf2 is the major transcription factor that regulates many of the cytoprotective enzymes involved in the adaptive stress response. Modulation of Nrf2 could be therapeutically useful in a number of disease states. Activation can occur through either an electrophilic or non-electrophilic mechanism. To date, most of the research has focused on electrophilic Nrf2 activators, but there is increasing interest in non-electrophilic modulators of Nrf2. This Digest examines the current selection of small molecules that modulate Nrf2 through non-electrophilic mechanisms, and it highlights new opportunities for this important therapeutic target. |
| doi_str_mv | 10.1016/j.bmcl.2015.04.019 |
| format | article |
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Nrf2 is the major transcription factor that regulates many of the cytoprotective enzymes involved in the adaptive stress response. Modulation of Nrf2 could be therapeutically useful in a number of disease states. Activation can occur through either an electrophilic or non-electrophilic mechanism. To date, most of the research has focused on electrophilic Nrf2 activators, but there is increasing interest in non-electrophilic modulators of Nrf2. This Digest examines the current selection of small molecules that modulate Nrf2 through non-electrophilic mechanisms, and it highlights new opportunities for this important therapeutic target.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2015.04.019</identifier><identifier>PMID: 25937010</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Adaptive stress response ; Cul3 ; Humans ; Intracellular Signaling Peptides and Proteins - genetics ; Intracellular Signaling Peptides and Proteins - metabolism ; Keap1 ; Kelch-Like ECH-Associated Protein 1 ; Models, Molecular ; NF-E2-Related Factor 2 - agonists ; NF-E2-Related Factor 2 - genetics ; NF-E2-Related Factor 2 - metabolism ; Nrf2 ; Nrf2 activator ; Nrf2 repressor ; Nrf2/Keap1 interaction ; Protein Binding ; Protein Conformation ; Protein–protein interaction ; Signal Transduction - drug effects</subject><ispartof>Bioorganic & medicinal chemistry letters, 2015-06, Vol.25 (11), p.2261-2268</ispartof><rights>2015 Elsevier Ltd</rights><rights>Copyright © 2015 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c591t-cfad3895d8ff62204bd9eac13bd1778f016c1d106e34626ff88567fedddee5e03</citedby><cites>FETCH-LOGICAL-c591t-cfad3895d8ff62204bd9eac13bd1778f016c1d106e34626ff88567fedddee5e03</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,314,780,784,885,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25937010$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Richardson, B.G.</creatorcontrib><creatorcontrib>Jain, A.D.</creatorcontrib><creatorcontrib>Speltz, T.E.</creatorcontrib><creatorcontrib>Moore, T.W.</creatorcontrib><title>Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
Nrf2 is the major transcription factor that regulates many of the cytoprotective enzymes involved in the adaptive stress response. Modulation of Nrf2 could be therapeutically useful in a number of disease states. Activation can occur through either an electrophilic or non-electrophilic mechanism. To date, most of the research has focused on electrophilic Nrf2 activators, but there is increasing interest in non-electrophilic modulators of Nrf2. This Digest examines the current selection of small molecules that modulate Nrf2 through non-electrophilic mechanisms, and it highlights new opportunities for this important therapeutic target.</description><subject>Adaptive stress response</subject><subject>Cul3</subject><subject>Humans</subject><subject>Intracellular Signaling Peptides and Proteins - genetics</subject><subject>Intracellular Signaling Peptides and Proteins - metabolism</subject><subject>Keap1</subject><subject>Kelch-Like ECH-Associated Protein 1</subject><subject>Models, Molecular</subject><subject>NF-E2-Related Factor 2 - agonists</subject><subject>NF-E2-Related Factor 2 - genetics</subject><subject>NF-E2-Related Factor 2 - metabolism</subject><subject>Nrf2</subject><subject>Nrf2 activator</subject><subject>Nrf2 repressor</subject><subject>Nrf2/Keap1 interaction</subject><subject>Protein Binding</subject><subject>Protein Conformation</subject><subject>Protein–protein interaction</subject><subject>Signal Transduction - drug effects</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><recordid>eNp9kEFP3DAQha2qqCy0f6AHlGMvCePEcWIJVVSoBQSCC5V6s7z2uOuVEwc7C-Lf16sFVC6c5jDvvXnzEfKVQkWB8uN1tRy0r2qgbQWsAio-kAVlnJUNg_YjWYDgUPaC_dknBymtASgDxj6R_boVTQcUFuT0JowletRzDNPKeaeLIZiNV3OIqQi2mFdYaDWG0WnliytUEz2-ibYuJjWvHtXTZ7JnlU_45Xkekt-_ft6dXZTXt-eXZz-uS90KOpfaKtP0ojW9tbyugS2NQKVpszS063qb_9HUUODYMF5za_u-5Z1FYwxii9Acku-73GmzHNBoHOeovJyiG1R8kkE5-XYzupX8Gx5k5tEI1uWAb88BMdxvMM1ycEmj92rEsEmSctHmKk29ldY7qY4hpYj29QwFuUUv13KLXm7RS2Ayo8-mo_8LvlpeWGfByU6AGdODwyiTdjhqNC5m_tIE917-P_U2log</recordid><startdate>20150601</startdate><enddate>20150601</enddate><creator>Richardson, B.G.</creator><creator>Jain, A.D.</creator><creator>Speltz, T.E.</creator><creator>Moore, T.W.</creator><general>Elsevier Ltd</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>5PM</scope></search><sort><creationdate>20150601</creationdate><title>Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway</title><author>Richardson, B.G. ; Jain, A.D. ; Speltz, T.E. ; Moore, T.W.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c591t-cfad3895d8ff62204bd9eac13bd1778f016c1d106e34626ff88567fedddee5e03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Adaptive stress response</topic><topic>Cul3</topic><topic>Humans</topic><topic>Intracellular Signaling Peptides and Proteins - genetics</topic><topic>Intracellular Signaling Peptides and Proteins - metabolism</topic><topic>Keap1</topic><topic>Kelch-Like ECH-Associated Protein 1</topic><topic>Models, Molecular</topic><topic>NF-E2-Related Factor 2 - agonists</topic><topic>NF-E2-Related Factor 2 - genetics</topic><topic>NF-E2-Related Factor 2 - metabolism</topic><topic>Nrf2</topic><topic>Nrf2 activator</topic><topic>Nrf2 repressor</topic><topic>Nrf2/Keap1 interaction</topic><topic>Protein Binding</topic><topic>Protein Conformation</topic><topic>Protein–protein interaction</topic><topic>Signal Transduction - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Richardson, B.G.</creatorcontrib><creatorcontrib>Jain, A.D.</creatorcontrib><creatorcontrib>Speltz, T.E.</creatorcontrib><creatorcontrib>Moore, T.W.</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>PubMed Central (Full Participant titles)</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Richardson, B.G.</au><au>Jain, A.D.</au><au>Speltz, T.E.</au><au>Moore, T.W.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2015-06-01</date><risdate>2015</risdate><volume>25</volume><issue>11</issue><spage>2261</spage><epage>2268</epage><pages>2261-2268</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
Nrf2 is the major transcription factor that regulates many of the cytoprotective enzymes involved in the adaptive stress response. Modulation of Nrf2 could be therapeutically useful in a number of disease states. Activation can occur through either an electrophilic or non-electrophilic mechanism. To date, most of the research has focused on electrophilic Nrf2 activators, but there is increasing interest in non-electrophilic modulators of Nrf2. This Digest examines the current selection of small molecules that modulate Nrf2 through non-electrophilic mechanisms, and it highlights new opportunities for this important therapeutic target.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>25937010</pmid><doi>10.1016/j.bmcl.2015.04.019</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2015-06, Vol.25 (11), p.2261-2268 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_4643947 |
| source | Elsevier |
| subjects | Adaptive stress response Cul3 Humans Intracellular Signaling Peptides and Proteins - genetics Intracellular Signaling Peptides and Proteins - metabolism Keap1 Kelch-Like ECH-Associated Protein 1 Models, Molecular NF-E2-Related Factor 2 - agonists NF-E2-Related Factor 2 - genetics NF-E2-Related Factor 2 - metabolism Nrf2 Nrf2 activator Nrf2 repressor Nrf2/Keap1 interaction Protein Binding Protein Conformation Protein–protein interaction Signal Transduction - drug effects |
| title | Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway |
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