Development of novel linkers to conjugate pharmacophores to a carrier antibody

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• 作者：Moorthy S.S. Palanki ; ^{moorthy.palanki@pfizer.com} ; Abhijit Bhat ; Rodney W. Lappe ; Bin Liu ; Bryan Oates ; John Rizzo ; Nebojsa Stankovic ; Curt Bradshaw
• 关键词：Linkers ; Bioconjugation ; Synthesis of novel linkers
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 July, 2012
• 卷：22
• 期：13
• 页码：4249-4253
• 文件大小：730 K

摘要

We have developed modified maleimide novel linkers with improved chemical stability that could potentially be used in conjugating various pharmacophores such as oligo nucleotides, peptides, and proteins to antibodies to afford novel biologics with well-defined therapeutic benefits and improved pharmacokinetic properties. These linkers expand the array of tools available for bioconjugation of pharmacophores to antibodies.