Università degli Studi di Milano, Dipartimento di Chimica, Via C. Golgi, 19 I-20133, Milan, Italy.
Org Biomol Chem. 2019 May 15;17(19):4705-4710. doi: 10.1039/c9ob00617f.
A non-internalizing αvβ3 integrin ligand was conjugated to the anticancer drug MMAE through a β-glucuronidase-responsive linker. In the presence of β-glucuronidase, only the conjugate bearing a PEG4 spacer inhibited the proliferation of integrin-expressing cancer cells at low nanomolar concentrations, indicating important structural requirements for the efficacy of these therapeutics.
一种非内化的αvβ3 整联蛋白配体通过β-葡萄糖醛酸酶响应性连接子与抗癌药物 MMAE 连接。在β-葡萄糖醛酸酶存在的情况下，只有带有 PEG4 间隔物的缀合物能够以低纳摩尔浓度抑制表达整联蛋白的癌细胞的增殖，这表明这些治疗药物的功效具有重要的结构要求。
