Synthesis and Biological Evaluation of Homogeneous Thiol‐Linked NHC*‐Au‐Albumin and ‐Trastuzumab Bioconjugates

Targeted delivery of potent cytotoxic drugs to cancer cells minimizes systemic toxicity and several side effects. NHC*−Au−Cl has already been proven to be a potent anticancer agent. In this study, we explore a strategy based on chemoselective cysteine conjugation of NHC*−Au−Cl to albumin and trastuz...

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Autores principales: Matos, Maria J., Labão‐Almeida, Carlos, Sayers, Claire, Dada, Oyinlola, Tacke, Matthias, Bernardes, Gonçalo J. L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2018
Materias:
Communications
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6120520/
https://www.ncbi.nlm.nih.gov/pubmed/29729206
http://dx.doi.org/10.1002/chem.201800872
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author Matos, Maria J.
Labão‐Almeida, Carlos
Sayers, Claire
Dada, Oyinlola
Tacke, Matthias
Bernardes, Gonçalo J. L.
author_facet Matos, Maria J.
Labão‐Almeida, Carlos
Sayers, Claire
Dada, Oyinlola
Tacke, Matthias
Bernardes, Gonçalo J. L.
author_sort Matos, Maria J.
collection PubMed
description Targeted delivery of potent cytotoxic drugs to cancer cells minimizes systemic toxicity and several side effects. NHC*−Au−Cl has already been proven to be a potent anticancer agent. In this study, we explore a strategy based on chemoselective cysteine conjugation of NHC*−Au−Cl to albumin and trastuzumab (Thiomab LC‐V205C) to potentiate drug‐ligand ratio, pharmacokinetics, as well as drug efficacy and safety. This strategy is a step forward towards the use of gold‐based anticancer agents as targeted therapies.
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spelling pubmed-61205202018-09-05 Synthesis and Biological Evaluation of Homogeneous Thiol‐Linked NHC*‐Au‐Albumin and ‐Trastuzumab Bioconjugates Matos, Maria J. Labão‐Almeida, Carlos Sayers, Claire Dada, Oyinlola Tacke, Matthias Bernardes, Gonçalo J. L. Chemistry Communications Targeted delivery of potent cytotoxic drugs to cancer cells minimizes systemic toxicity and several side effects. NHC*−Au−Cl has already been proven to be a potent anticancer agent. In this study, we explore a strategy based on chemoselective cysteine conjugation of NHC*−Au−Cl to albumin and trastuzumab (Thiomab LC‐V205C) to potentiate drug‐ligand ratio, pharmacokinetics, as well as drug efficacy and safety. This strategy is a step forward towards the use of gold‐based anticancer agents as targeted therapies. John Wiley and Sons Inc. 2018-05-22 2018-08-22 /pmc/articles/PMC6120520/ /pubmed/29729206 http://dx.doi.org/10.1002/chem.201800872 Text en © 2018 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
spellingShingle Communications
Matos, Maria J.
Labão‐Almeida, Carlos
Sayers, Claire
Dada, Oyinlola
Tacke, Matthias
Bernardes, Gonçalo J. L.
Synthesis and Biological Evaluation of Homogeneous Thiol‐Linked NHC*‐Au‐Albumin and ‐Trastuzumab Bioconjugates
title Synthesis and Biological Evaluation of Homogeneous Thiol‐Linked NHC*‐Au‐Albumin and ‐Trastuzumab Bioconjugates
title_full Synthesis and Biological Evaluation of Homogeneous Thiol‐Linked NHC*‐Au‐Albumin and ‐Trastuzumab Bioconjugates
title_fullStr Synthesis and Biological Evaluation of Homogeneous Thiol‐Linked NHC*‐Au‐Albumin and ‐Trastuzumab Bioconjugates
title_full_unstemmed Synthesis and Biological Evaluation of Homogeneous Thiol‐Linked NHC*‐Au‐Albumin and ‐Trastuzumab Bioconjugates
title_short Synthesis and Biological Evaluation of Homogeneous Thiol‐Linked NHC*‐Au‐Albumin and ‐Trastuzumab Bioconjugates
title_sort synthesis and biological evaluation of homogeneous thiol‐linked nhc*‐au‐albumin and ‐trastuzumab bioconjugates
topic Communications
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6120520/
https://www.ncbi.nlm.nih.gov/pubmed/29729206
http://dx.doi.org/10.1002/chem.201800872
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