期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 17, 期 7, 页码 1869-1874出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8ob01798k
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资金
- National Research Foundation of Korea [2018R1A2B6004479]
- National Research Foundation of Korea [2018R1A2B6004479] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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 C7functionalization of DMXAA would be applicable to access other C7-substituted DMXAA analogues as potential hSTING agonists.
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