Department of Chemistry, New York University, New York, New York 10003, USA.
Org Biomol Chem. 2013 Jul 7;11(25):4142-6. doi: 10.1039/c3ob40606g.
We report the first example of chemoselective fragment condensation, through native amide bond formation, between peptoid and peptide oligomers. Peptoid oligomers bearing C-terminal salicylaldehyde esters were synthesized and ligated to peptides containing N-terminal serine or threonine residues. We investigate the ligation efficiency of peptoid oligomers varying in length, sequence, and C-terminal steric bulk. These protocols enhance accessibility of structurally complex peptoid-peptide hybrids and will facilitate the design new semi-synthetic proteins with unique attributes.
我们报告了首例通过酰胺键的选择性片段缩合，实现肽和肽寡聚物之间的化学选择性连接。我们合成了带有末端水杨醛酯的肽寡聚物，并将其连接到含有 N 末端丝氨酸或苏氨酸残基的肽上。我们研究了长度、序列和末端空间位阻不同的肽寡聚物的连接效率。这些方案提高了结构复杂的肽-肽杂合体的可及性，并将促进具有独特属性的新型半合成蛋白的设计。
