Heinis Christian
Ecole Polytechnique Fédérale de Lausanne, EPFL Institute of Chemical Sciences and Engineering, CH1015 Lausanne.
Chimia (Aarau). 2011;65(9):677-9. doi: 10.2533/chimia.2011.677.
Ligands based on bicyclic peptides can combine favourable properties of antibodies (good binding affinity and target specificity) and small molecule ligands (stability, access to chemical synthesis, diffusion properties) and might be suitable molecular structures for the development of therapeutics. By using a combinatorial methodology based on phage display and a chemical cyclisation reaction, we are generating bicyclic peptide antagonists of protein targets with therapeutic applications in mind.
基于双环肽的配体可以结合抗体的有利特性（良好的结合亲和力和靶标特异性）和小分子配体的特性（稳定性、可进行化学合成、扩散特性），可能是开发治疗药物的合适分子结构。通过使用基于噬菌体展示和化学环化反应的组合方法，我们正在生成针对蛋白质靶标的双环肽拮抗剂，并将治疗应用考虑在内。
