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Divinylpyrimidine reagents generate antibody-drug conjugates with excellent in vivo efficacy and tolerability.


ABSTRACT: The development of divinylpyrimidine (DVP) reagents for the synthesis of antibody-drug conjugates (ADCs) with in vivo efficacy and tolerability is reported. Detailed structural characterisation of the synthesised ADCs was first conducted followed by in vitro and in vivo evaluation of the ADCs' ability to safely and selectively eradicate target-positive tumours.

SUBMITTER: Walsh SJ 

PROVIDER: S-EPMC9073851 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature

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Divinylpyrimidine reagents generate antibody-drug conjugates with excellent <i>in vivo</i> efficacy and tolerability.

Walsh Stephen J SJ   Omarjee Soleilmane S   Dannheim Friederike M FM   Couturier Dominique-Laurent DL   Bexheti Dorentina D   Mendil Lee L   Cronshaw Gemma G   Fewster Toby T   Gregg Charlotte C   Brodie Cara C   Miller Jodi L JL   Houghton Richard R   Carroll Jason S JS   Spring David R DR  

Chemical communications (Cambridge, England) 20220208 12


The development of divinylpyrimidine (DVP) reagents for the synthesis of antibody-drug conjugates (ADCs) with <i>in vivo</i> efficacy and tolerability is reported. Detailed structural characterisation of the synthesised ADCs was first conducted followed by <i>in vitro</i> and <i>in vivo</i> evaluation of the ADCs' ability to safely and selectively eradicate target-positive tumours. ...[more]

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