Synthesis and Biological Evaluation of Homogeneous Thiol-Linked NHC*-Au-Albumin and -Trastuzumab Bioconjugates.
Published version
Peer-reviewed
Repository URI
Repository DOI
Change log
Authors
Matos, Maria J https://orcid.org/0000-0002-3470-8299
Labão-Almeida, Carlos
Sayers, Claire
Dada, Oyinlola
Tacke, Matthias
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.
Description
Keywords
albumin, anticancer drug, drug delivery, gold(I) complex, targeted therapeutics, Antineoplastic Agents, Cell Line, Tumor, Cell Survival, Cysteine, Drug Carriers, Gold, Half-Life, Humans, Imidazolines, Serum Albumin, Sulfhydryl Compounds, Trastuzumab
Journal Title
Chemistry
Conference Name
Journal ISSN
0947-6539
1521-3765
1521-3765
Volume Title
24
Publisher
Wiley
Publisher DOI
Sponsorship
Engineering and Physical Sciences Research Council (EP/M003647/1)
The Royal Society (uf110046)
European Research Council (676832)
European Commission (EC) (852985)
The Royal Society (uf110046)
European Research Council (676832)
European Commission (EC) (852985)