Nunes João P M, Morais Maurício, Vassileva Vessela, Robinson Eifion, Rajkumar Vineeth S, Smith Mark E B, Pedley R Barbara, Caddick Stephen, Baker James R, Chudasama Vijay
Department of Chemistry, University College London, London, WC1H 0AJ, UK.
Chem Commun (Camb). 2015 Jul 7;51(53):10624-7. doi: 10.1039/c5cc03557k. Epub 2015 Jun 5.
Herein we report the use of next generation maleimides (NGMs) for the construction of a potent antibody-drug conjugate (ADC) via functional disulfide bridging. The linker has excellent stability in blood serum and the ADC, armed with monomethyl auristatin E (MMAE), shows excellent potency and cancer cell selectivity in vitro.
在此,我们报道了通过功能性二硫键桥连使用下一代马来酰亚胺(NGM)构建强效抗体-药物偶联物(ADC)。该连接子在血清中具有出色的稳定性,且装载单甲基澳瑞他汀E(MMAE)的ADC在体外表现出优异的效力和癌细胞选择性。