Synthesis and Vaccine Evaluation of the Tumor Associated by Hong-Yang Chuang

By Hong-Yang Chuang

This thesis specializes in the synthesis and vaccine overview of the prostate tumor- linked carbohydrate antigen RM2. the writer first provides using the [1+2+3] one-pot sequential technique to effectively synthesise the RM2 antigen and its analogues as unmarried stereoisomers in each glycosylation step, generating solid yields and stereoselectivity. He then introduces the conjugation of the unreal RM2 antigen to the provider protein CRM197 in an ordinary variety of 1–10 to create the prostate melanoma vaccine candidate, that is mixed with α-galactosylceramide C1, its analogue C34, or Alu. the result of the vaccination reviews in mice also are defined and point out that the most powerful anti-RM2 antigen titer is exhibited while one molecule of diphtheria toxin (DT) is conjugated with a normal of 4.7 molecules of RM2 antigen (DT-RM4.7) and adjuvanted with the glycolipid C34. extra importantly, the brought on mouse antibodies mediate the powerful complement-dependent cytotoxicity (CDC) opposed to the prostate melanoma phone line LNCap. The examine offered during this thesis is the 1st ever to effectively synthesize this complicated glycan molecule. because of the steric difficulty of the adjoining sialyl moiety, the creation of 2 sialic acid devices to the compact and inflexible 3,4 di branched galactoside unit is particularly hard and the β-selective and effective glycosylation of the galactosamine moiety on the 4-position of di branched galactose is usually problematic.

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