Camperi Silvia A, Giudicessi Silvana L, Martínez-Ceron María C, Gurevich-Messina Juan M, Saavedra Soledad L, Acosta Gerardo, Cascone Osvaldo, Erra-Balsells Rosa, Albericio Fernando
NANOBIOTEC Institute, UBA-CONICET, Cathedra of Biotechnology, School of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina.
National Scientific and Technological Research Council (CONICET), Buenos Aires, Argentina.
Curr Protoc Chem Biol. 2016 Jun 2;8(2):109-130. doi: 10.1002/cpch.2.
Combinatorial library screening coupled to mass spectrometry (MS) analysis is a practical approach to identify useful peptides. Cyclic peptides can have high biological activity, selectivity, and affinity for target proteins, and high stability against proteolytic degradation. Here we describe two strategies to prepare combinatorial libraries suitable for MS analysis to accelerate the discovery of cyclic peptide structures. Both approaches use ChemMatrix resin and the linker 4-hydroxymethylbenzoic acid. One strategy involves the synthesis of a one-bead-two-peptides library in which each bead contains both the cyclic peptide and its linear counterpart to facilitate MS analysis. The other protocol is based on the synthesis of a cyclic depsipeptide library in which a glycolamidic ester group is incorporated by adding glycolic acid. After library screening, the ring is opened and the peptide is released simultaneously for subsequent MS analysis. © 2016 by John Wiley & Sons, Inc.
组合文库筛选与质谱（MS）分析相结合是鉴定有用肽段的一种实用方法。环肽对靶蛋白可具有高生物活性、选择性和亲和力，并且对蛋白水解降解具有高稳定性。在此，我们描述两种制备适用于MS分析的组合文库的策略，以加速环肽结构的发现。两种方法均使用ChemMatrix树脂和连接子4-羟甲基苯甲酸。一种策略涉及合成单珠双肽文库，其中每个珠子同时包含环肽及其线性对应物，以利于MS分析。另一种方案基于环缩肽文库的合成，其中通过添加乙醇酸引入甘醇酰胺酯基团。文库筛选后，环打开，肽同时释放以便进行后续的MS分析。© 2016约翰威立国际出版公司
