The Department of Chemistry and Biochemistry, University of South Carolina , Columbia, South Carolina 29208, United States.
ACS Comb Sci. 2011 May 9;13(3):232-43. doi: 10.1021/co100054e. Epub 2011 Mar 25.
Aberrant glycosylation of cell membrane and secreted glycoproteins is a hallmark of various disease states, including cancer. The natural lectins currently used in the recognition of these glycoproteins are costly, difficult to produce, and unstable toward rigorous use. Herein we describe the design and synthesis of several boronic acid functionalized peptide-based synthetic lectin (SL) libraries, as well as the optimized methodology for obtaining peptide sequences of these SLs. SL libraries were subsequently used to identify SLs with as high as 5-fold selectivity for various glycoproteins. SLs will inevitably find a role in cancer diagnostics, given that they do not suffer from the drawbacks of natural lectins and that the combinatorial nature of these libraries allows for the identification of an SL for nearly any glycosylated biomolecule.
细胞膜和分泌型糖蛋白的异常糖基化是多种疾病状态的标志，包括癌症。目前用于识别这些糖蛋白的天然凝集素成本高、难以生产，并且在严格使用时不稳定。在此，我们描述了几种硼酸功能化肽基合成凝集素（SL）文库的设计和合成，以及获得这些 SL 的肽序列的优化方法。随后，使用 SL 文库来鉴定对各种糖蛋白具有高达 5 倍选择性的 SL。鉴于 SL 没有天然凝集素的缺点，并且这些文库的组合性质允许鉴定几乎任何糖基化生物分子的 SL，因此 SL 必将在癌症诊断中发挥作用。
