Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy
We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). Compounds 5, 6, and 7 induced cIAP1-mediated ubiquitylation of ERα resulting in its proteasomal degradation.
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2012-02, Vol.22 (4), p.1793-1796 |
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| container_end_page | 1796 |
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| container_issue | 4 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 22 |
| creator | Demizu, Yosuke Okuhira, Keiichiro Motoi, Hiromi Ohno, Akiko Shoda, Takuji Fukuhara, Kiyoshi Okuda, Haruhiro Naito, Mikihiko Kurihara, Masaaki |
| description | We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). Compounds 5, 6, and 7 induced cIAP1-mediated ubiquitylation of ERα resulting in its proteasomal degradation. |
| doi_str_mv | 10.1016/j.bmcl.2011.11.086 |
| format | Article |
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Compounds 5, 6, and 7 induced cIAP1-mediated ubiquitylation of ERα resulting in its proteasomal degradation.</description><subject>Antineoplastic Agents - pharmacology</subject><subject>apoptosis</subject><subject>Biological and medical sciences</subject><subject>Breast Neoplasms</subject><subject>Cell Line, Tumor</subject><subject>chemistry</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Design</subject><subject>Estrogen receptor</subject><subject>Estrogen Receptor alpha - metabolism</subject><subject>estrogen receptors</subject><subject>Female</subject><subject>Humans</subject><subject>Inhibitor of Apoptosis Proteins - metabolism</subject><subject>Medical sciences</subject><subject>Models, Biological</subject><subject>Molecular Structure</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Binding</subject><subject>Protein knockdown</subject><subject>Receptors, Estrogen - metabolism</subject><subject>Tamoxifen</subject><subject>Ubiquitin-proteasome system</subject><subject>Ubiquitination - drug effects</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kUuLFDEQgIMo7uzqH_CgucieekzSnaQbvMj6hAUPuuAtpJNKm9meZEx6lPn31jCj3oSCkPDVI18R8oyzNWdcvdqsx62b14JxvsZgvXpAVrxTXdN2TD4kKzYo1vRD9-2CXNa6YYx3rOsekwshhNZCqxVxb6HGKVGbPK2HtHzHa6U5UKhLyRMkWsDBbsmFepiK9XaJOdGY_N5BoaOt4Ck-WLoreYGY6H3K7t7nX4liBbvAdHhCHgU7V3h6Pq_I3ft3X28-NrefP3y6eXPbOMn00vB-VGz0rdZh0KFnIyg-cB78IJXiI3NKgFOKBQhOai57qYVkfLQw8ND60F6R61NdHOXHHj9gtrE6mGebIO-rGUTLB9lrhaQ4ka7kWgsEsytxa8vBcGaObs3GHN2ao1uDgW4x6fm5_H7cgv-b8kcmAi_PgK3OzqHY5GL9x0klNLLIvThxwWZjp4LM3RfsJHFBrWKtROL1iQDU9TNCMdVFSA58xHUsxuf4v0l_A_icodU</recordid><startdate>20120215</startdate><enddate>20120215</enddate><creator>Demizu, Yosuke</creator><creator>Okuhira, Keiichiro</creator><creator>Motoi, Hiromi</creator><creator>Ohno, Akiko</creator><creator>Shoda, Takuji</creator><creator>Fukuhara, Kiyoshi</creator><creator>Okuda, Haruhiro</creator><creator>Naito, Mikihiko</creator><creator>Kurihara, Masaaki</creator><general>Elsevier Ltd</general><general>Elsevier</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20120215</creationdate><title>Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy</title><author>Demizu, Yosuke ; Okuhira, Keiichiro ; Motoi, Hiromi ; Ohno, Akiko ; Shoda, Takuji ; Fukuhara, Kiyoshi ; Okuda, Haruhiro ; Naito, Mikihiko ; Kurihara, Masaaki</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c507t-18b60bd377f97f80be61911fd95661b0c62ec660fefc57158572501bae91f3df3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Antineoplastic Agents - pharmacology</topic><topic>apoptosis</topic><topic>Biological and medical sciences</topic><topic>Breast Neoplasms</topic><topic>Cell Line, Tumor</topic><topic>chemistry</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Design</topic><topic>Estrogen receptor</topic><topic>Estrogen Receptor alpha - metabolism</topic><topic>estrogen receptors</topic><topic>Female</topic><topic>Humans</topic><topic>Inhibitor of Apoptosis Proteins - metabolism</topic><topic>Medical sciences</topic><topic>Models, Biological</topic><topic>Molecular Structure</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Binding</topic><topic>Protein knockdown</topic><topic>Receptors, Estrogen - metabolism</topic><topic>Tamoxifen</topic><topic>Ubiquitin-proteasome system</topic><topic>Ubiquitination - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Demizu, Yosuke</creatorcontrib><creatorcontrib>Okuhira, Keiichiro</creatorcontrib><creatorcontrib>Motoi, Hiromi</creatorcontrib><creatorcontrib>Ohno, Akiko</creatorcontrib><creatorcontrib>Shoda, Takuji</creatorcontrib><creatorcontrib>Fukuhara, Kiyoshi</creatorcontrib><creatorcontrib>Okuda, Haruhiro</creatorcontrib><creatorcontrib>Naito, Mikihiko</creatorcontrib><creatorcontrib>Kurihara, Masaaki</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>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>Demizu, Yosuke</au><au>Okuhira, Keiichiro</au><au>Motoi, Hiromi</au><au>Ohno, Akiko</au><au>Shoda, Takuji</au><au>Fukuhara, Kiyoshi</au><au>Okuda, Haruhiro</au><au>Naito, Mikihiko</au><au>Kurihara, Masaaki</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2012-02-15</date><risdate>2012</risdate><volume>22</volume><issue>4</issue><spage>1793</spage><epage>1796</epage><pages>1793-1796</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). 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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2012-02, Vol.22 (4), p.1793-1796 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Antineoplastic Agents - pharmacology apoptosis Biological and medical sciences Breast Neoplasms Cell Line, Tumor chemistry Dose-Response Relationship, Drug Drug Design Estrogen receptor Estrogen Receptor alpha - metabolism estrogen receptors Female Humans Inhibitor of Apoptosis Proteins - metabolism Medical sciences Models, Biological Molecular Structure Pharmacology. Drug treatments Protein Binding Protein knockdown Receptors, Estrogen - metabolism Tamoxifen Ubiquitin-proteasome system Ubiquitination - drug effects |
| title | Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy |
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