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Direct Comparison of Linear and Macrocyclic Compound Libraries as a Source of Protein Ligands

机译：线性和大环化合物库作为蛋白质配体来源的直接比较

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摘要

There has been much discussion of the potential desirability of macrocyclic molecules for the development of tool compounds and drug leads. But there is little experimental data comparing otherwise equivalent macrocyclic and linear compound libraries as a source of protein ligands. In this Letter, we probe this point in the context of peptoid libraries. Bead-displayed libraries of macrocyclic and linear peptoids containing four variable positions and 0-2 fixed residues, to vary the ring size, were screened against streptavidin and the affinity of every hit for the target was measured. The data show that macrocyclization is advantageous, but only when the ring contains 17 atoms, not 20 or 23 atoms. This technology will be useful for conducting direct comparisons between many different types of chemical libraries to determine their relative utility as a source of protein ligands.
机译：对于开发工具化合物和药物前导物的大环分子的潜在需求，已有很多讨论。但是，几乎没有实验数据可以比较等同的大环和线性化合物库作为蛋白质配体的来源。在这封信中，我们在类肽库的背景下探讨了这一点。针对链霉亲和素筛选了含有四个可变位置和0-2个固定残基（可改变环大小）的大环和线性类肽的珠子展示文库，并针对链霉亲和素进行了筛选，并测定了每次命中靶标的亲和力。数据表明大环化是有利的，但是仅当环包含17个原子而不是20或23个原子时。该技术可用于在许多不同类型的化学文库之间进行直接比较，以确定它们作为蛋白质配体来源的相对效用。

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