CHEM564 Lecture Notes - Lecture 3: Glycosylation, Cytotoxicity, Trastuzumab

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Document Summary

A classic problem in medicinal and biological chemistry is the targeting of drug molecules to specific cell types. The ability to control the location of a drug molecule would allow for the restriction of toxic side-effects. For example, an anti-cancer therapeutic which has systemic toxicity could have reduced side effects if it only targeted the cell type that was cancerous. This idea was probably first enunciated by ehrlich as the magic bullet approach. 12 bioconjugate chemistry has often been applied to this problem, with perhaps the most common strategy involving the use of monoclonal antibodies to provide specificity. General descriptions of antibody structure are available elsewhere. xi reviews of the major issues that face the development of new adc are available. 13, 14. Unmodified antibodies are proteins which can be derivitized using chemical strategies outlined in section ii. Acylation reagents, such as carbodiimides (e. g. edci) are often the first choice for these strategies.