Development of novel linkers to conjugate pharmacophores to a carrier antibody

被引：19

作者：

Palanki, Moorthy S. S. ^{[1
]}

Bhat, Abhijit ^{[1
]}

Lappe, Rodney W. ^{[1
]}

Liu, Bin ^{[1
]}

Oates, Bryan ^{[1
]}

Rizzo, John ^{[1
]}

Stankovic, Nebojsa ^{[1
]}

Bradshaw, Curt ^{[1
]}

机构：

[1] Pfizer Worldwide Res & Dev, CovX Res, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 13期

关键词：

Linkers; Bioconjugation; Synthesis of novel linkers; HYDROLYSIS; SUCCINIMIDE; GENERATION; MALEIMIDES; ALKALINE; KINETICS; ACID;

D O I：

10.1016/j.bmcl.2012.05.040

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：4249 / 4253

页数：5

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