NHC*-Gold(I) Bioconjugated to Carbohydrates and Peptides as Targeted Anticancer Drugs
07 June 2019
11T09:20:22Z June 2019
Targeted delivery of potent cytotoxic drugs to cancer cells minimizes systemic toxicity and potentially avoids side effects. NHC*-Au-Cl has already been proven to be a potent anticancer agent based on the stabilising and lipophilic properties of the 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene (NHC*) ligand. One possibility is the chemoselective thiosugar conjugation to NHC*-Au-Cl in order to have active uptake of the resulting NHC*-Au-SR primarily into tumour tissue through the Warburg effect. In addition, a strategy based on chemoselective cysteine conjugation of NHC*-Au-Cl to human serum albumin or Trastuzumab to potentiate drug-ligand ratio, pharmacokinetics, as well as drug efficacy and safety is presented. These strategies are essential steps forward towards the use of gold-based anticancer agents as targeted therapies.
University College Dublin
School of Chemistry at UCD
National Cancer Institute in Maryland (USA).
Type of Material
Press of Slovak University of Technology, Bratislava
Monograph Series of the International Conferences on Coordination and Bioinorganic Chemistry held periodically at Smolenice in Slovakia
Copyright (Published Version)
2019 Slovak Chemical Society, Bratislava
Status of Item
Melník, M., Segľa, P., Tatarko, M. (eds.). Progressive trends in coordination, bioinorganic, and applied inorganic chemistry
XXVII International Conference on Coordination and Bioinorganic Chemistry, Bratislava, Slovakia, 2-7 June 2019
This item is made available under a Creative Commons License