Pinilla C, Appel J, Blondelle S, Dooley C, Dörner B, Eichler J, Ostresh J, Houghten R A
Torrey Pines Institute for Molecular Studies, San Diego, CA 92121.
Biopolymers. 1995;37(3):221-40. doi: 10.1002/bip.360370306.
This paper reviews the preparation and use of soluble synthetic combinatorial libraries (SCLs) made up of millions of peptide and nonpeptide sequences for the identification of highly active individual compounds. First presented in 1991, SCLs have been prepared in a number of different lengths and formats, and are composed entirely of L-, D-, and unnatural amino acids. Also, existing peptide libraries have been chemically transformed to yield large diversities of nonpeptidic compounds. This review encompasses the published work from this laboratory using SCLs for the identification of antigenic sequences recognized by monoclonal antibodies, novel peptide agonists and antagonists to opioid receptors, new trypsin inhibitors, novel antibacterials, and compounds that inhibit melittin's hemolytic activity. SCLs offer a fundamental, practical advance in the study of interactions between peptide and nonpeptide sequences and their biochemical or pharmacological targets.
本文综述了由数百万个肽和非肽序列组成的可溶性合成组合文库（SCL）的制备和应用，旨在识别高活性的单个化合物。SCL于1991年首次提出，已制备出多种不同长度和形式，且完全由L-、D-和非天然氨基酸组成。此外，现有的肽文库已通过化学转化产生大量不同的非肽化合物。本综述涵盖了本实验室发表的利用SCL识别单克隆抗体识别的抗原序列、阿片受体的新型肽激动剂和拮抗剂、新型胰蛋白酶抑制剂、新型抗菌剂以及抑制蜂毒溶血活性的化合物的研究工作。SCL为肽和非肽序列与其生化或药理学靶点之间相互作用的研究提供了一项基础性的实际进展。
