Robinson, E;
Nunes, JPM;
Vassileva, V;
Maruani, A;
Nogueira, JCF;
Smith, MEB;
Pedley, RB;
... Chudasama, V; + view all
(2017)
Pyridazinediones deliver potent, stable, targeted and efficacious antibody–drug conjugates (ADCs) with a controlled loading of 4 drugs per antibody.
RSC Advances
, 7
(15)
pp. 9073-9077.
10.1039/C7RA00788D.
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Abstract
Herein we report the use of pyridazinediones to functionalise the native solvent accessible interstrand disulfide bonds in trastuzumab with monomethyl auristatin E (MMAE). This method of conjugation delivers serum stable antibody–drug conjugates (ADCs) with a controlled drug loading of 4. Moreover, we demonstrate that the MMAE-bearing ADCs are potent, selective and efficacious against cancer cell lines in both in vitro and in vivo models.
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