Non-platinum anti-cancer drugs Flashcards
What is the most important factor to consider with metals in medicine?
Speed of ligand exchange
What is the key problem with Au(III) complexes?
Reduction of Au(III) to Au(I) rapid under cellular conditions.
How can we overcome the problems with Au(III) complexes?
Use strongly sigma donating ligands or rigid multidentate ligands
What mode of action do Au(I) complexes use?
Au (I) complexes bind to Se in the active site of TrxR, responsible for redox control. By inhibiting activity of this enzyme, cell apoptosis is triggered.
How can you activate Ru(III) complexes to become active drug molecules in the body?
Ru(III) rapidly reduced to Ru(II) in biological media. Rate of ligand exchange for Ru(II) significantly faster than Ru(III).
How can you use fluorescence techniques to investigate drug activity?
Usage of ethidium bromide intercalation displacement assays. Positive charge is solvated in water and fluorescence is quenched. Will intercalate between base pairs and fluorescence no longer quenched. Adding intercalating drugs produces competition - less fluorescence seen.
How do inert complexes work as therapeutics?
Using 3D nature of complexes to block active site of enzymes. Makes them ideal for efficient and selective binding to enzymes.
What are three different ways drugs could act in the body?
Binding to key parts of the function of an enzyme, antimetastatic (prevents spread of cancer cells - mechanism unknown but likely protein binding) or cytotoxicity (binds to something in cell which leads to cell death).
