Robinson John A
Chemistry Department, University of Zürich, Switzerland.
Chembiochem. 2009 Apr 17;10(6):971-3. doi: 10.1002/cbic.200900055.
On the scaffold: Grafting protein epitopes onto conformationally designed scaffolds represents a very promising approach to protein ligand design, with potential applications in many areas of chemical biology and molecular medicine. The highlighted article describes the design and anticancer activity of novel p53/MDM2 inhibitors built upon a scorpion toxin scaffold. Other approaches to protein epitope mimetics are also briefly discussed.
将蛋白质表位嫁接到构象设计的支架上是蛋白质配体设计中一种非常有前景的方法,在化学生物学和分子医学的许多领域都有潜在应用。这篇重点文章描述了基于蝎毒素支架构建的新型p53/MDM2抑制剂的设计及其抗癌活性。还简要讨论了蛋白质表位模拟物的其他方法。