DC Field | Value | Language |
---|---|---|
dc.contributor.author | Hwang, Jihyun | ko |
dc.contributor.author | Kang, Taeho | ko |
dc.contributor.author | Lee, Janghyun | ko |
dc.contributor.author | Choi, Byong-Seok | ko |
dc.contributor.author | Han, Sunkyu | ko |
dc.date.accessioned | 2019-02-20T05:12:26Z | - |
dc.date.available | 2019-02-20T05:12:26Z | - |
dc.date.created | 2018-12-11 | - |
dc.date.created | 2018-12-11 | - |
dc.date.created | 2018-12-11 | - |
dc.date.issued | 2019-02 | - |
dc.identifier.citation | ORGANIC & BIOMOLECULAR CHEMISTRY, v.17, no.7, pp.1869 - 1874 | - |
dc.identifier.issn | 1477-0520 | - |
dc.identifier.uri | http://hdl.handle.net/10203/250363 | - |
dc.description.abstract | STING, a central protein in the innate immune response to cytosolic DNA, has emerged as a hot target for the development of vaccine-adjuvants and anticancer drugs. The discovery of potent human-STING (hSTING) agonist is expected to revolutionize the current cancer immunotherapy. Inspired by the X-ray crystal structure of DMXAA (5,6-dimethylxanthenone-4-acetic acid) and hSTINGG230I complex, we designed various DMXAA derivatives that contain a hydrogen bonding donor/acceptor or a halide at the C7 position. While 7-bromo- and 7-hydroxyl-DMXAA showed notable binding to mouse-STING (mSTING), our newly synthesized C7-functionalized DMXAA derivatives did not bind to hSTING. Nevertheless, our newly developed synthetic protocol for the C7-functionalization of DMXAA would be applicable to access other C7-substituted DMXAA analogues as potential hSTING agonists. | - |
dc.language | English | - |
dc.publisher | ROYAL SOC CHEMISTRY | - |
dc.title | Design, synthesis, and biological evaluation of C7-functionalized DMXAA derivatives as potential human-STING agonists | - |
dc.type | Article | - |
dc.identifier.wosid | 000458679200041 | - |
dc.identifier.scopusid | 2-s2.0-85061515830 | - |
dc.type.rims | ART | - |
dc.citation.volume | 17 | - |
dc.citation.issue | 7 | - |
dc.citation.beginningpage | 1869 | - |
dc.citation.endingpage | 1874 | - |
dc.citation.publicationname | ORGANIC & BIOMOLECULAR CHEMISTRY | - |
dc.identifier.doi | 10.1039/c8ob01798k | - |
dc.contributor.localauthor | Choi, Byong-Seok | - |
dc.contributor.localauthor | Han, Sunkyu | - |
dc.contributor.nonIdAuthor | Kang, Taeho | - |
dc.description.isOpenAccess | N | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordPlus | CATALYZED HYDROXYLATION | - |
dc.subject.keywordPlus | ANTITUMOR AGENTS | - |
dc.subject.keywordPlus | INNATE | - |
dc.subject.keywordPlus | DNA | - |
dc.subject.keywordPlus | ANALOGS | - |
dc.subject.keywordPlus | MOUSE | - |
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