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

Maria João MatosCarlos Labão-AlmeidaClaire SayersOyinlola DadaMatthias TackeGonçalo J L Bernardes

Published in: Chemistry (Weinheim an der Bergstrasse, Germany) (2018)

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.

Keyphrases

sensitive detection
reduced graphene oxide
epidermal growth factor receptor
drug induced
metastatic breast cancer
anti inflammatory
oxidative stress
adverse drug
mass spectrometry
quantum dots
emergency department
simultaneous determination
tyrosine kinase
fluorescent probe
liquid chromatography