Full synthesis and bioactivity evaluation of Tn-RC-529 derivative conjugates as self-adjuvanting cancer vaccines

• Published in: Chinese chemical letters Vol. 32; no. 10; pp. 3011 - 3014
• Main Authors: Gao, Lingqiang, Lian, Qinghai, Ma, Leilei, Su, Shiwei, Yang, Menglan, Fang, Yuan, Liu, Zhongqiu, Luo, Xiang, Liao, Guochao
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.10.2021; Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education,International Institute for Translational Chinese Medicine,Guangzhou University of Chinese Medicine,Guangzhou 510006,China
• Subjects: Cancer vaccines; Glycoconjugates; RC-529; Tn antigen; Cancer vaccines; RC-529; Tn antigen; Glycoconjugates
• ISSN: 1001-8417; 1878-5964
• DOI: 10.1016/j.cclet.2021.03.046

Tn-based vaccines carried by RC-529 derivatives were synthesized and elicited strongly T cell-dependent immune responses without external adjuvants. The antisera induced by these conjugates could specifically recognize, bind to and kill Tn-overexpressing cancer cells. [Display omitted] A facile and efficient strategy was established for the construction of RC-529 and its derivatives. Four conjugates of RC-529 derivatives with Tn antigen were synthesized and all elicited strong and T cell-dependent immune responses in mice without requiring external adjuvants. In addition, all antisera induced by these conjugates could specifically recognize, bind to and kill Tn-overexpressing cancer cells. Thus, RC-529 shows promise as a useful platform for the development of new vaccine carriers with self-adjuvanting properties for the treatment of cancer. Moreover, preliminary structure-activity relationship analysis provides convincing support for further optimization of, and additional investigation into, RC-529.