High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139
Aim： To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules. Methods： Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies. Results： Five small molecule ant...
Gespeichert in:
| Veröffentlicht in: | Acta pharmacologica Sinica 2015-07, Vol.36 (7), p.874-878 |
|---|---|
| Hauptverfasser: | , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 878 |
|---|---|
| container_issue | 7 |
| container_start_page | 874 |
| container_title | Acta pharmacologica Sinica |
| container_volume | 36 |
| creator | Wang, Jia Zhu, Lin-yun Liu, Qing Hentzer, Morten Smith, Garrick Paul Wang, Ming-wei |
| description | Aim： To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules. Methods： Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies. Results： Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds. Conclusion： The findings provide important tools for further study of this orphan G-protein coupled receptor. |
| doi_str_mv | 10.1038/aps.2015.12 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_4648122</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><cqvip_id>665568159</cqvip_id><sourcerecordid>1693706799</sourcerecordid><originalsourceid>FETCH-LOGICAL-c473t-983c0d934808aeb2852d842e180e304768292593cd7bd5110d085ae8c81a0b5e3</originalsourceid><addsrcrecordid>eNptkc2LFDEQxRtR3HX15F2CXgTtMZV0PvoiyKKzwoIievAUMuma7l56kt4kLfjfm3HGYRVPCdSv3quqV1VPga6Acv3GzmnFKIgVsHvVOahG1IqJ5n75SwV1QzU_qx6ldEMpZxzah9UZk5QpKeG8-n419kOdhxiWfpiXTJKLiH70PQlbYn22ffBjyolsQyR5QBLiPFhP1vUcQ8bRExeWecKORHQ450KtP38B3j6uHmztlPDJ8b2ovn14__Xyqr7-tP54-e66do3iuW41d7RreaOptrhhWrBONwxBU-S0UVKzlomWu05tOgFAO6qFRe00WLoRyC-qtwfdednssHPoc7STmeO4s_GnCXY0f1f8OJg-_DCNbDQwVgReHgViuF0wZbMbk8Npsh7DkgzIlisqVdsW9MU_6E1Yoi_r_aZAAwhRqFcHysWQUsTtaRigZh-ZKZGZfWQG9vbP7s5_Yv9kVIDXByCVku8x3jH9r97zo_sQfH9bOk6SUgohNZRr_gKTYqty</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1693181155</pqid></control><display><type>article</type><title>High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139</title><source>MEDLINE</source><source>PubMed Central</source><source>Alma/SFX Local Collection</source><creator>Wang, Jia ; Zhu, Lin-yun ; Liu, Qing ; Hentzer, Morten ; Smith, Garrick Paul ; Wang, Ming-wei</creator><creatorcontrib>Wang, Jia ; Zhu, Lin-yun ; Liu, Qing ; Hentzer, Morten ; Smith, Garrick Paul ; Wang, Ming-wei</creatorcontrib><description>Aim： To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules. Methods： Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies. Results： Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds. Conclusion： The findings provide important tools for further study of this orphan G-protein coupled receptor.</description><identifier>ISSN: 1671-4083</identifier><identifier>EISSN: 1745-7254</identifier><identifier>DOI: 10.1038/aps.2015.12</identifier><identifier>PMID: 26027661</identifier><language>eng</language><publisher>London: Nature Publishing Group UK</publisher><subject>Animals ; Biomedical and Life Sciences ; Biomedicine ; Calcium - metabolism ; CHO Cells ; Cricetinae ; Cricetulus ; Dose-Response Relationship, Drug ; Drug Evaluation, Preclinical - methods ; High-Throughput Screening Assays - methods ; Humans ; Immunology ; Internal Medicine ; Medical Microbiology ; Nerve Tissue Proteins - antagonists & inhibitors ; Nerve Tissue Proteins - metabolism ; Original ; original-article ; Pharmacology/Toxicology ; Receptors, G-Protein-Coupled - antagonists & inhibitors ; Receptors, G-Protein-Coupled - metabolism ; Vaccine ; 受体拮抗剂 ; 合成化合物 ; 吞吐量 ; 孤儿G蛋白偶联受体 ; 小分子 ; 钙动员 ; 高通量筛选</subject><ispartof>Acta pharmacologica Sinica, 2015-07, Vol.36 (7), p.874-878</ispartof><rights>CPS and SIMM 2015</rights><rights>Copyright Nature Publishing Group Jul 2015</rights><rights>Copyright © 2015 CPS and SIMM 2015 CPS and SIMM</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c473t-983c0d934808aeb2852d842e180e304768292593cd7bd5110d085ae8c81a0b5e3</citedby><cites>FETCH-LOGICAL-c473t-983c0d934808aeb2852d842e180e304768292593cd7bd5110d085ae8c81a0b5e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Uhttp://image.cqvip.com/vip1000/qk/95561A/95561A.jpg</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4648122/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4648122/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,315,728,781,785,886,27929,27930,53796,53798</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/26027661$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Wang, Jia</creatorcontrib><creatorcontrib>Zhu, Lin-yun</creatorcontrib><creatorcontrib>Liu, Qing</creatorcontrib><creatorcontrib>Hentzer, Morten</creatorcontrib><creatorcontrib>Smith, Garrick Paul</creatorcontrib><creatorcontrib>Wang, Ming-wei</creatorcontrib><title>High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139</title><title>Acta pharmacologica Sinica</title><addtitle>Acta Pharmacol Sin</addtitle><addtitle>Acta Pharmacologica Sinica</addtitle><description>Aim： To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules. Methods： Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies. Results： Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds. Conclusion： The findings provide important tools for further study of this orphan G-protein coupled receptor.</description><subject>Animals</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Calcium - metabolism</subject><subject>CHO Cells</subject><subject>Cricetinae</subject><subject>Cricetulus</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Evaluation, Preclinical - methods</subject><subject>High-Throughput Screening Assays - methods</subject><subject>Humans</subject><subject>Immunology</subject><subject>Internal Medicine</subject><subject>Medical Microbiology</subject><subject>Nerve Tissue Proteins - antagonists & inhibitors</subject><subject>Nerve Tissue Proteins - metabolism</subject><subject>Original</subject><subject>original-article</subject><subject>Pharmacology/Toxicology</subject><subject>Receptors, G-Protein-Coupled - antagonists & inhibitors</subject><subject>Receptors, G-Protein-Coupled - metabolism</subject><subject>Vaccine</subject><subject>受体拮抗剂</subject><subject>合成化合物</subject><subject>吞吐量</subject><subject>孤儿G蛋白偶联受体</subject><subject>小分子</subject><subject>钙动员</subject><subject>高通量筛选</subject><issn>1671-4083</issn><issn>1745-7254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNptkc2LFDEQxRtR3HX15F2CXgTtMZV0PvoiyKKzwoIievAUMuma7l56kt4kLfjfm3HGYRVPCdSv3quqV1VPga6Acv3GzmnFKIgVsHvVOahG1IqJ5n75SwV1QzU_qx6ldEMpZxzah9UZk5QpKeG8-n419kOdhxiWfpiXTJKLiH70PQlbYn22ffBjyolsQyR5QBLiPFhP1vUcQ8bRExeWecKORHQ450KtP38B3j6uHmztlPDJ8b2ovn14__Xyqr7-tP54-e66do3iuW41d7RreaOptrhhWrBONwxBU-S0UVKzlomWu05tOgFAO6qFRe00WLoRyC-qtwfdednssHPoc7STmeO4s_GnCXY0f1f8OJg-_DCNbDQwVgReHgViuF0wZbMbk8Npsh7DkgzIlisqVdsW9MU_6E1Yoi_r_aZAAwhRqFcHysWQUsTtaRigZh-ZKZGZfWQG9vbP7s5_Yv9kVIDXByCVku8x3jH9r97zo_sQfH9bOk6SUgohNZRr_gKTYqty</recordid><startdate>20150701</startdate><enddate>20150701</enddate><creator>Wang, Jia</creator><creator>Zhu, Lin-yun</creator><creator>Liu, Qing</creator><creator>Hentzer, Morten</creator><creator>Smith, Garrick Paul</creator><creator>Wang, Ming-wei</creator><general>Nature Publishing Group UK</general><general>Nature Publishing Group</general><scope>2RA</scope><scope>92L</scope><scope>CQIGP</scope><scope>W91</scope><scope>~WA</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>3V.</scope><scope>7QP</scope><scope>7QR</scope><scope>7T5</scope><scope>7TK</scope><scope>7TO</scope><scope>7U9</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8FD</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>H94</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M7N</scope><scope>M7P</scope><scope>P64</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>7X8</scope><scope>5PM</scope></search><sort><creationdate>20150701</creationdate><title>High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139</title><author>Wang, Jia ; Zhu, Lin-yun ; Liu, Qing ; Hentzer, Morten ; Smith, Garrick Paul ; Wang, Ming-wei</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c473t-983c0d934808aeb2852d842e180e304768292593cd7bd5110d085ae8c81a0b5e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Animals</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Calcium - metabolism</topic><topic>CHO Cells</topic><topic>Cricetinae</topic><topic>Cricetulus</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Evaluation, Preclinical - methods</topic><topic>High-Throughput Screening Assays - methods</topic><topic>Humans</topic><topic>Immunology</topic><topic>Internal Medicine</topic><topic>Medical Microbiology</topic><topic>Nerve Tissue Proteins - antagonists & inhibitors</topic><topic>Nerve Tissue Proteins - metabolism</topic><topic>Original</topic><topic>original-article</topic><topic>Pharmacology/Toxicology</topic><topic>Receptors, G-Protein-Coupled - antagonists & inhibitors</topic><topic>Receptors, G-Protein-Coupled - metabolism</topic><topic>Vaccine</topic><topic>受体拮抗剂</topic><topic>合成化合物</topic><topic>吞吐量</topic><topic>孤儿G蛋白偶联受体</topic><topic>小分子</topic><topic>钙动员</topic><topic>高通量筛选</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Wang, Jia</creatorcontrib><creatorcontrib>Zhu, Lin-yun</creatorcontrib><creatorcontrib>Liu, Qing</creatorcontrib><creatorcontrib>Hentzer, Morten</creatorcontrib><creatorcontrib>Smith, Garrick Paul</creatorcontrib><creatorcontrib>Wang, Ming-wei</creatorcontrib><collection>中文科技期刊数据库</collection><collection>中文科技期刊数据库-CALIS站点</collection><collection>中文科技期刊数据库-7.0平台</collection><collection>中文科技期刊数据库-医药卫生</collection><collection>中文科技期刊数据库- 镜像站点</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Immunology Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Oncogenes and Growth Factors Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>Technology Research Database</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection (ProQuest)</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Engineering Research Database</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Biological Science Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Acta pharmacologica Sinica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Wang, Jia</au><au>Zhu, Lin-yun</au><au>Liu, Qing</au><au>Hentzer, Morten</au><au>Smith, Garrick Paul</au><au>Wang, Ming-wei</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139</atitle><jtitle>Acta pharmacologica Sinica</jtitle><stitle>Acta Pharmacol Sin</stitle><addtitle>Acta Pharmacologica Sinica</addtitle><date>2015-07-01</date><risdate>2015</risdate><volume>36</volume><issue>7</issue><spage>874</spage><epage>878</epage><pages>874-878</pages><issn>1671-4083</issn><eissn>1745-7254</eissn><abstract>Aim： To discover antagonists of the orphan G-protein coupled receptor GPR139 through high-throughput screening of a collection of diverse small molecules. Methods： Calcium mobilization assays were used to identify initial hits and for subsequent confirmation studies. Results： Five small molecule antagonists, representing 4 different scaffolds, were identified following high-throughput screening of 16 000 synthetic compounds. Conclusion： The findings provide important tools for further study of this orphan G-protein coupled receptor.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>26027661</pmid><doi>10.1038/aps.2015.12</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1671-4083 |
| ispartof | Acta pharmacologica Sinica, 2015-07, Vol.36 (7), p.874-878 |
| issn | 1671-4083 1745-7254 |
| language | eng |
| recordid | cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_4648122 |
| source | MEDLINE; PubMed Central; Alma/SFX Local Collection |
| subjects | Animals Biomedical and Life Sciences Biomedicine Calcium - metabolism CHO Cells Cricetinae Cricetulus Dose-Response Relationship, Drug Drug Evaluation, Preclinical - methods High-Throughput Screening Assays - methods Humans Immunology Internal Medicine Medical Microbiology Nerve Tissue Proteins - antagonists & inhibitors Nerve Tissue Proteins - metabolism Original original-article Pharmacology/Toxicology Receptors, G-Protein-Coupled - antagonists & inhibitors Receptors, G-Protein-Coupled - metabolism Vaccine 受体拮抗剂 合成化合物 吞吐量 孤儿G蛋白偶联受体 小分子 钙动员 高通量筛选 |
| title | High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139 |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-13T09%3A57%3A26IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_pubme&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=High-throughput%20screening%20of%20antagonists%20for%20the%20orphan%20G-protein%20coupled%20receptor%20GPR139&rft.jtitle=Acta%20pharmacologica%20Sinica&rft.au=Wang,%20Jia&rft.date=2015-07-01&rft.volume=36&rft.issue=7&rft.spage=874&rft.epage=878&rft.pages=874-878&rft.issn=1671-4083&rft.eissn=1745-7254&rft_id=info:doi/10.1038/aps.2015.12&rft_dat=%3Cproquest_pubme%3E1693706799%3C/proquest_pubme%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=1693181155&rft_id=info:pmid/26027661&rft_cqvip_id=665568159&rfr_iscdi=true |