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

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’ abili...

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Autores principales: Walsh, Stephen J., Omarjee, Soleilmane, Dannheim, Friederike M., Couturier, Dominique-Laurent, Bexheti, Dorentina, Mendil, Lee, Cronshaw, Gemma, Fewster, Toby, Gregg, Charlotte, Brodie, Cara, Miller, Jodi L., Houghton, Richard, Carroll, Jason S., Spring, David R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9073851/
https://www.ncbi.nlm.nih.gov/pubmed/35044383
http://dx.doi.org/10.1039/d1cc06766d
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author Walsh, Stephen J.
Omarjee, Soleilmane
Dannheim, Friederike M.
Couturier, Dominique-Laurent
Bexheti, Dorentina
Mendil, Lee
Cronshaw, Gemma
Fewster, Toby
Gregg, Charlotte
Brodie, Cara
Miller, Jodi L.
Houghton, Richard
Carroll, Jason S.
Spring, David R.
author_facet Walsh, Stephen J.
Omarjee, Soleilmane
Dannheim, Friederike M.
Couturier, Dominique-Laurent
Bexheti, Dorentina
Mendil, Lee
Cronshaw, Gemma
Fewster, Toby
Gregg, Charlotte
Brodie, Cara
Miller, Jodi L.
Houghton, Richard
Carroll, Jason S.
Spring, David R.
author_sort Walsh, Stephen J.
collection PubMed
description 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.
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spelling pubmed-90738512022-05-27 Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability Walsh, Stephen J. Omarjee, Soleilmane Dannheim, Friederike M. Couturier, Dominique-Laurent Bexheti, Dorentina Mendil, Lee Cronshaw, Gemma Fewster, Toby Gregg, Charlotte Brodie, Cara Miller, Jodi L. Houghton, Richard Carroll, Jason S. Spring, David R. Chem Commun (Camb) Chemistry 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. The Royal Society of Chemistry 2022-01-13 /pmc/articles/PMC9073851/ /pubmed/35044383 http://dx.doi.org/10.1039/d1cc06766d Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by/3.0/
spellingShingle Chemistry
Walsh, Stephen J.
Omarjee, Soleilmane
Dannheim, Friederike M.
Couturier, Dominique-Laurent
Bexheti, Dorentina
Mendil, Lee
Cronshaw, Gemma
Fewster, Toby
Gregg, Charlotte
Brodie, Cara
Miller, Jodi L.
Houghton, Richard
Carroll, Jason S.
Spring, David R.
Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability
title Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability
title_full Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability
title_fullStr Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability
title_full_unstemmed Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability
title_short Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability
title_sort divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9073851/
https://www.ncbi.nlm.nih.gov/pubmed/35044383
http://dx.doi.org/10.1039/d1cc06766d
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