Department of Pediatric Oncology, Dana-Farber Cancer Institute , Boston, Massachusetts 02215, United States.
ACS Chem Biol. 2014 Mar 21;9(3):831-7. doi: 10.1021/cb4003305. Epub 2014 Jan 3.
Hydrocarbon stapling is a chemical approach to restoring and fortifying the natural α-helical structure of peptides that otherwise unfold when taken out of context from the host protein. By iterating the peptide sequence, staple type, and sites of insertion, discrete compositions can be generated to suit a diversity of biochemical, structural, proteomic, cellular, and drug development applications. Here, we reinforce key design considerations to avoid pitfalls and maximize progress when applying stapled peptides in chemistry and biology research.
烃 stapling 是一种化学方法，用于恢复和加强肽的天然 α-螺旋结构，否则当从宿主蛋白中取出时，肽会展开。通过迭代肽序列、 stapler 类型和插入位置，可以生成离散的组合物，以适应多种生化、结构、蛋白质组学、细胞和药物开发应用。在这里，我们加强了关键的设计考虑因素，以避免在化学和生物学研究中应用 stapled 肽时出现陷阱并最大程度地推进研究。
