Just David, Palivec Vladimír, Bártová Kateřina, Bednárová Lucie, Pazderková Markéta, Císařová Ivana, Martinez-Seara Hector, Jahn Ullrich
Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Flemingovo náměstí 2, 16610, Prague 6, Czech Republic.
Department of Inorganic Chemistry, Faculty of Science, Charles University in Prague, Hlavova 2030/8, 12843, Prague 2, Czech Republic.
Commun Chem. 2024 May 25;7(1):114. doi: 10.1038/s42004-024-01201-7.
Peptide-like foldamers controlled by normal amide backbone hydrogen bonding have been extensively studied, and their folding patterns largely rely on configurational and conformational constraints induced by the steric properties of backbone substituents at appropriate positions. In contrast, opportunities to influence peptide secondary structure by functional groups forming individual hydrogen bond networks have not received much attention. Here, peptide-like foldamers consisting of alternating α,β,γ-triamino acids 3-amino-4-(aminomethyl)-2-methylpyrrolidine-3-carboxylate (AAMP) and natural amino acids glycine and alanine are reported, which were obtained by solution phase peptide synthesis. They form ordered secondary structures, which are dominated by a three-dimensional bridged triazaspiranoid-like hydrogen bond network involving the non-backbone amino groups, the backbone amide hydrogen bonds, and the relative configuration of the α,β,γ-triamino and α-amino acid building blocks. This additional stabilization leads to folding in both nonpolar organic as well as in aqueous environments. The three-dimensional arrangement of the individual foldamers is supported by X-ray crystallography, NMR spectroscopy, chiroptical methods, and molecular dynamics simulations.
由正常酰胺主链氢键控制的类肽折叠体已得到广泛研究,其折叠模式很大程度上依赖于在适当位置的主链取代基的空间性质所诱导的构型和构象限制。相比之下,通过形成单个氢键网络的官能团来影响肽二级结构的机会尚未受到太多关注。在此,报道了由交替的α,β,γ-三氨基酸3-氨基-4-(氨甲基)-2-甲基吡咯烷-3-羧酸酯(AAMP)与天然氨基酸甘氨酸和丙氨酸组成的类肽折叠体,它们通过溶液相肽合成获得。它们形成有序的二级结构,其主要由涉及非主链氨基、主链酰胺氢键以及α,β,γ-三氨基酸和α-氨基酸构建单元的相对构型的三维桥连三氮杂螺环类氢键网络主导。这种额外的稳定性导致在非极性有机环境以及水性环境中均发生折叠。通过X射线晶体学、核磁共振光谱、手性光学方法和分子动力学模拟对各个折叠体的三维排列进行了证实。