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Development of Small-Molecule STING Activators for Cancer Immunotherapy

التفاصيل البيبلوغرافية
العنوان: Development of Small-Molecule STING Activators for Cancer Immunotherapy
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
الوصف
تدمد:10010033
22279059
DOI:10.3390/biomedicines10010033