Gunnoo Smita B, Madder Annemieke
Organic and Biomimetic Chemistry Research Group, Department of Organic and Macromolecular Chemistry, Ghent University, Krijgslaan 281, Ghent, 9000, Belgium.
Org Biomol Chem. 2016 Sep 14;14(34):8002-13. doi: 10.1039/c6ob00808a. Epub 2016 Jul 27.
The pharmaceutical market has largely been dominated by small molecule drugs; however, larger biomolecules have recently become important contenders. Of these biomolecules, protein and peptide therapeutics are proving useful due to their often improved pharmacokinetic properties. In many circumstances, functionalisation of the protein or peptide therapeutics results in performance enhancement, and various methodologies are applied. In addition, introducing unnatural amino acids for structural reinforcement via chemical modification is also common. These strategies are discussed in this review.
制药市场在很大程度上一直由小分子药物主导;然而,更大的生物分子最近已成为重要的竞争者。在这些生物分子中,蛋白质和肽类疗法因其通常改善的药代动力学特性而被证明是有用的。在许多情况下,蛋白质或肽类疗法的功能化会导致性能增强,并应用了各种方法。此外,通过化学修饰引入非天然氨基酸以增强结构也很常见。本综述将讨论这些策略。