دورية أكاديمية
Development of Small-Molecule STING Activators for Cancer Immunotherapy
العنوان: | Development of Small-Molecule STING Activators for Cancer Immunotherapy |
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المؤلفون: | Hee Ra Jung, Seongman Jo, Min Jae Jeon, Hyelim Lee, Yeonjeong Chu, Jeehee Lee, Eunha Kim, Gyu Yong Song, Cheulhee Jung, Hyejin Kim, Sanghee Lee |
المصدر: | Biomedicines, Vol 10, Iss 1, p 33 (2021) |
بيانات النشر: | MDPI AG, 2021. |
سنة النشر: | 2021 |
المجموعة: | LCC:Biology (General) |
مصطلحات موضوعية: | cancer immunotherapy, type I interferon, STING, STING activator, Biology (General), QH301-705.5 |
الوصف: | 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. |
نوع الوثيقة: | article |
وصف الملف: | electronic resource |
اللغة: | English |
تدمد: | 10010033 2227-9059 |
Relation: | https://www.mdpi.com/2227-9059/10/1/33; https://doaj.org/toc/2227-9059 |
DOI: | 10.3390/biomedicines10010033 |
URL الوصول: | https://doaj.org/article/dbeb9309e5e44ec4b35bde18670bf92a |
رقم الأكسشن: | edsdoj.beb9309e5e44ec4b35bde18670bf92a |
قاعدة البيانات: | Directory of Open Access Journals |
تدمد: | 10010033 22279059 |
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DOI: | 10.3390/biomedicines10010033 |