Development of Small-Molecule STING Activators for Cancer Immunotherapy
DC Field | Value | Language |
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dc.contributor.author | Jung, Hee Ra | - |
dc.contributor.author | Jo, Seongman | - |
dc.contributor.author | Jeon, Min Jae | - |
dc.contributor.author | Lee, Hyelim | - |
dc.contributor.author | Chu, Yeonjeong | - |
dc.contributor.author | Lee, Jeehee | - |
dc.contributor.author | Kim, Eunha | - |
dc.contributor.author | Song, Gyu Yong | - |
dc.contributor.author | Jung, Cheulhee | - |
dc.contributor.author | Kim, Hyejin | - |
dc.contributor.author | Lee, Sanghee | - |
dc.date.accessioned | 2022-03-02T20:41:38Z | - |
dc.date.available | 2022-03-02T20:41:38Z | - |
dc.date.created | 2022-03-02 | - |
dc.date.issued | 2022-01 | - |
dc.identifier.issn | 2227-9059 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/137540 | - |
dc.description.abstract | In cancer immunotherapy, the cyclic GMP-AMP synthase-stimulator of interferon genes (STING) pathway is an attractive target for switching the tumor immunophenotype from 'cold' to 'hot' through the activation of the type I interferon response. To develop a new chemical entity for STING activator to improve cyclic GMP-AMP (cGAMP)-induced innate immune response, we identified KAS-08 via the structural modification of DW2282, which was previously reported as an anti-cancer agent with an unknown mechanism. Further investigation revealed that direct STING binding or the enhanced phosphorylation of STING and downstream effectors were responsible for DW2282-or KAS-08-mediated STING activity. Furthermore, KAS-08 was validated as an effective STING pathway activator in vitro and in vivo. The synergistic effect of cGAMP-mediated immunity and efficient anti-cancer effects successfully demonstrated the therapeutic potential of KAS-08 for combination therapy in cancer treatment. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | MDPI | - |
dc.subject | IMMUNE CHECKPOINT BLOCKADE | - |
dc.subject | I INTERFERON | - |
dc.subject | PHASE-II | - |
dc.subject | DNA | - |
dc.subject | EFFICACY | - |
dc.subject | DW2282 | - |
dc.subject | AGENT | - |
dc.title | Development of Small-Molecule STING Activators for Cancer Immunotherapy | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Jung, Cheulhee | - |
dc.identifier.doi | 10.3390/biomedicines10010033 | - |
dc.identifier.scopusid | 2-s2.0-85121812375 | - |
dc.identifier.wosid | 000747824900001 | - |
dc.identifier.bibliographicCitation | BIOMEDICINES, v.10, no.1 | - |
dc.relation.isPartOf | BIOMEDICINES | - |
dc.citation.title | BIOMEDICINES | - |
dc.citation.volume | 10 | - |
dc.citation.number | 1 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Research & Experimental Medicine | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Medicine, Research & Experimental | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.subject.keywordPlus | IMMUNE CHECKPOINT BLOCKADE | - |
dc.subject.keywordPlus | I INTERFERON | - |
dc.subject.keywordPlus | PHASE-II | - |
dc.subject.keywordPlus | DNA | - |
dc.subject.keywordPlus | EFFICACY | - |
dc.subject.keywordPlus | DW2282 | - |
dc.subject.keywordPlus | AGENT | - |
dc.subject.keywordAuthor | cancer immunotherapy | - |
dc.subject.keywordAuthor | type I interferon | - |
dc.subject.keywordAuthor | STING | - |
dc.subject.keywordAuthor | STING activator | - |
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