Mal-VC-PAB-DM1 is a drug-linker conjugate used in the construction of antibody-drug conjugates (ADCs). Mal-VC-PAB-DM1 specifically couples with sulfhydryl groups on antibodies via maleimide (Mal) moiety. After the formed ADC enters tumor cells, the Val-Cit dipeptide linker is cleaved by lysosomal proteases, thereby releasing the potent tubulin inhibitor DM1 to kill tumor cells. For instance, T-DM1 has been successfully applied in treating HER2-positive breast cancer, demonstrating the potential of ADC drugs in targeted tumor therapy[1].
References:
[1] Gedik ME, Saatci O, Oberholtzer N, et al. Targeting TACC3 Induces Immunogenic Cell Death and Enhances T-DM1 Response in HER2-Positive Breast Cancer. Cancer Res. 2024 May 2;84(9):1475-1490.
Mal-VC-PAB-DM1是一种用于构建抗体偶联药物（ADC）的药物-连接子偶联物。Mal-VC-PAB-DM1 可通过其马来酰亚胺（Mal）基团与抗体的巯基特异性偶联，形成的ADC在进入肿瘤细胞后，其Val-Cit二肽连接子可被溶酶体蛋白酶切割，从而释放出强效的微管蛋白抑制剂DM1，杀伤肿瘤细胞，如T-DM1已成功用于治疗HER2阳性乳腺癌，展现了ADC药物在肿瘤靶向治疗中的潜力[1]。