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本文从药物学前景的角度讨论了治疗蛋白在临床中应用的现状,着重分析开发这些化合物的药物学实践及其临床应用。许多“新”蛋白药物是通过DNA重组技术制备的,对它们全部的生物学作用尚了解甚少。临床上为了行之有效,其应用浓度及环境条件常明显不同于其自然类似物,无疑会给机体带来不必要的影响。因此常需通过改变蛋白的物理化学和生物学特性来避免、减少毒性及增加药效。所用的方法有:(1)与其它大分子物质形成共价结合;(2)与抗体结合,主要是物理性改良;(3)通过诱变除去蛋白中妨碍功能的结构部分;(4)糖基化。
This article discusses the clinical application of therapeutic proteins in the perspective of pharmacology and focuses on the pharmacological practice and clinical application of these compounds. Many of the “new” protein drugs are made by DNA recombination techniques and little is known about their overall biological role. Clinically, in order to be effective, its application concentration and environmental conditions often differ significantly from its natural analogues, will undoubtedly bring unnecessary impact to the body. Therefore often need to change the physical and chemical properties of proteins to avoid, reduce toxicity and increase efficacy. The methods used are: (1) formation of a covalent bond with other macromolecular species; (2) binding to an antibody, primarily physical modification; (3) removal of structurally impeded functions in the protein by mutagenesis; Based on.