title: Synthetic and immunological studies of N-acyl modified S-linked STn derivatives as anticancer vaccine candidates.
abstract: It is well known that tumor cells express some aberrant glycans, termed tumor-associated carbohydrate antigens (TACAs). TACAs are good targets for the development of carbohydrate-based anticancer vaccines. However, one of the major problems is that carbohydrate antigens possess a weak immunogenicity. To tackle this problem, a number of unnatural N-modified S-linked STn analogues were designed and prepared. Reaction of the modified STn disaccharides with bifunctional adipic acid p-nitrophenyl diester provided the corresponding activated esters, which was followed by the conjugation with keyhole limpet hemocyanin (KLH), affording the corresponding protein conjugates. The immunological properties of these glycoconjugates were evaluated in a mouse model. The results showed that the modified glycoconjugates stimulated the production of IgG antibodies that are capable of recognizing the naturally occurring STn antigen, helping the discovery of carbohydrate-based anticancer vaccine candidates.
authors: State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, and Center for Molecular and Translational Medicine, Peking University, Xue Yuan Rd No. 38, Beijing 100191, China. xinshan@bjmu.edu.cn.
authors: Chang-Xin
authors: CX
authors: Huo
authors: Xiu-Jing
authors: XJ
authors: Zheng
authors: An
authors: A
authors: Xiao
authors: Chang-Cheng
authors: CC
authors: Liu
authors: Shuang
authors: S
authors: Sun
authors: Zhuo
authors: Z
authors: Lv
authors: Xin-Shan
authors: XS
authors: Ye
mesh_terms: D000818:Animals; D015295:Antigens, Tumor-Associated, Carbohydrate / Q000737:chemistry / Q000276:immunology*; D019496:Cancer Vaccines / Q000276:immunology*; D005260:Female; D006001:Glycoconjugates / Q000138:chemical synthesis / Q000737:chemistry; D007114:Immunization; D008297:Male; D008807:Mice, Inbred BALB C
chemical_list: D015295:Antigens, Tumor-Associated, Carbohydrate; D019496:Cancer Vaccines; D006001:Glycoconjugates; C055491:sialosyl-Tn antigen