Owens R A, Gesellchen P D, Houchins B J, DiMarchi R D
Lilly Research Laboratories, Indianapolis, Indiana 46285.
Biochem Biophys Res Commun. 1991 Nov 27;181(1):402-8. doi: 10.1016/s0006-291x(05)81433-0.
Small peptides with activity as enzyme inhibitors, hormone antagonists, or other peptide mimetics, can be identified by synthesizing and screening large numbers of peptides as defined mixtures. Several coupling reactions, each with a different amino acid, can be conducted simultaneously and then combined to generate a near equimolar mixture before coupling additional residues. The peptide mixtures are recovered free from the matrix and in quantities sufficient for screening in many assays. We describe the rapid identification of a potent peptide inhibitor of human immunodeficiency virus protease from twenty-two mixtures containing more than 240,000 tetrapeptides.
具有酶抑制剂、激素拮抗剂或其他肽模拟物活性的小肽，可以通过合成和筛选大量定义好的肽混合物来鉴定。可以同时进行几种不同氨基酸的偶联反应，然后在偶联额外残基之前将它们合并以生成接近等摩尔的混合物。肽混合物可以从基质中回收，且回收量足以用于多种检测的筛选。我们描述了从二十二种含有超过240,000种四肽的混合物中快速鉴定出一种有效的人类免疫缺陷病毒蛋白酶肽抑制剂的过程。
