1,2,3-Triazoles as Amide Bond Mimics: Triazole Scan Yields Protease-Resistant Peptidomimetics for Tumor Targeting
1,2,3-Triazoles as Amide Bond Mimics: Triazole Scan Yields Protease-Resistant Peptidomimetics for Tumor Targeting
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DOI：
10.1002/anie.201303108
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发表时间：
2013-08-19
影响因子：
16.6
通讯作者：
Mindt, Thomas L.
中科院分区：
文献类型：
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作者：
Valverde, Ibai E.;Bauman, Andreas;Mindt, Thomas L.
三唑发挥了作用：用1，4-二取代的1，2，3-三唑等排体取代肽骨架中的酰胺键，提供了具有保留的受体亲和力和细胞内化特性、增强的蛋白水解稳定性和改善的肿瘤靶向能力的肽模拟物。
The triazole makes the difference: Replacement of amide bonds in the backbone of peptides by 1, 4‐disubstituted 1, 2, 3‐triazole isosteres affords peptidomimetics with retained receptor affinity and cell‐internalization properties, enhanced proteolytic stability, and improved tumor‐targeting capabilities.