Article
Controlled coupling of an ultrapotent auristatin warhead to cetuximab yields a next-generation antibody-drug conjugate for EGFR-targeted therapy of KRAS mutant pancreatic cancer.
British journal of cancer - 1 Nov 2020
Greene Michelle K, Chen Ting, Robinson Eifion, Straubinger Ninfa L, Minx Charlene, Chan Darren K W, Wang Jun, Burrows James F, Van Schaeybroeck Sandra, Baker James R, Caddick Stephen, Longley Daniel B, Mager Donald E, Straubinger Robert M, Chudasama Vijay, Scott Christopher J
Abstract excerpt
BACKGROUND: Antibody-drug conjugate (ADC) construction poses numerous challenges that limit clinical progress. In particular, common bioconjugation methods afford minimal control over the site of drug coupling to antibodies. Here, such difficulties are overcome through re-bridging of the inter-chain disulfides of cetuximab (CTX) with auristatin-bearing pyridazinediones, to yield a highly refined anti-epidermal...
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