Blanchfield Joanne T, Toth Istvan
School of Molecular and Microbial Sciences, University of Queensland, St Lucia, Australia.
Methods Mol Biol. 2005;298:45-61. doi: 10.1385/1-59259-877-3:045.
The scientific literature is full of new small molecules and larger peptides identified as potential pharmaceutical agents for a variety of diseases. The majority of these compounds, however, will never progress into the clinic because of poor oral absorption and low metabolic stability. The development of practical, economic, and widely applicable systems to improve the bioavailability of drugs is a highly sought-after goal. The conjugation of a drug with lipid and/or sugar units represents one of the most important strategies being investigated in this new field of drug delivery. This chapter describes one method of introducing lipidic groups to drugs via lipoamino acids and also provides useful procedures for the efficient incorporation of sugar units into drugs, particularly peptide drugs, via solid phase synthesis.
科学文献中充斥着大量被鉴定为可用于治疗多种疾病的潜在药物的新型小分子和较大的肽类。然而，这些化合物中的大多数由于口服吸收差和代谢稳定性低而永远无法进入临床阶段。开发实用、经济且广泛适用的系统以提高药物的生物利用度是一个备受追捧的目标。将药物与脂质和/或糖单元缀合是在这个新的药物递送领域中正在研究的最重要策略之一。本章描述了一种通过脂氨基酸将脂质基团引入药物的方法，还提供了通过固相合成将糖单元有效掺入药物（特别是肽类药物）的有用步骤。
