Department of Chemistry, University of Leicester, Leicester LE1 7RH, UK.
Chem Biol Drug Des. 2013 Jan;81(1):148-65. doi: 10.1111/cbdd.12042.
Peptide-based therapeutics have grown in importance over the last few decades. Furthermore, peptides have been extensively used as lead compounds in the drug discovery process to investigate the nature of chemical space required for molecular recognition and activity at a variety of targets. This critical commentary reviews scanning techniques, which employ natural and non-proteinogenic amino acids to facilitate understanding of structural requirements for peptide biological activity. The value of sequence analysis by such methods is highlighted by examples, in which the elements for peptide affinity and activity have been elucidated and employed to prepare peptidomimetic leads for drug development.
在过去的几十年中，基于肽的治疗方法的重要性日益增加。此外，肽已被广泛用作药物发现过程中的先导化合物，以研究在各种靶标中进行分子识别和活性所需的化学空间的性质。本评论批判性地回顾了扫描技术，该技术使用天然和非蛋白质氨基酸来促进对肽生物活性的结构要求的理解。通过实例强调了此类方法的序列分析的价值，其中已经阐明了肽亲和力和活性的要素，并将其用于制备用于药物开发的肽类似物先导物。
