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

ABSTRACT: 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.

SUBMITTER: Matos MJ

PROVIDER: S-EPMC6120520 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature

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

Matos Maria J MJ Labão-Almeida Carlos C Sayers Claire C Dada Oyinlola O Tacke Matthias M Bernardes Gonçalo J L GJL

Chemistry (Weinheim an der Bergstrasse, Germany) 20180522 47

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 targe ...[more]

PMID: 29729206

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