Rhenium and Technetium-oxo Complexes with Thioamide Derivatives of Pyridylhydrazine Bifunctional Chelators Conjugated to the Tumour Targeting Peptides Octreotate and Cyclic-RGDfK.
Andrea J NorthJohn A KarasMichelle T MaPhilip J BlowerUwe AckermannJonathan M WhitePaul S DonnellyPublished in: Inorganic chemistry (2017)
This research aimed to develop new tumor targeted theranostic agents taking advantage of the similarities in coordination chemistry between technetium and rhenium. A γ-emitting radioactive isotope of technetium is commonly used in diagnostic imaging, and there are two β- emitting radioactive isotopes of rhenium that have the potential to be of use in radiotherapy. Variants of the 6-hydrazinonicotinamide (HYNIC) bifunctional ligands have been prepared by appending thioamide functional groups to 6-hydrazinonicotinamide to form pyridylthiosemicarbazide ligands (SHYNIC). The new bidentate ligands were conjugated to the tumor targeting peptides Tyr3-octreotate and cyclic-RGD. The new ligands and conjugates were used to prepare well-defined {M═O}3+ complexes (where M = 99mTc or natRe or 188Re) that feature two targeting peptides attached to the single metal ion. These new SHYNIC ligands are capable of forming well-defined rhenium and technetium complexes and offer the possibility of using the 99mTc imaging and 188/186Re therapeutic matched pairs.
Keyphrases
- cancer therapy
- photodynamic therapy
- high resolution
- quantum dots
- fluorescence imaging
- radiation therapy
- amino acid
- drug delivery
- fluorescent probe
- copy number
- deep learning
- locally advanced
- risk assessment
- energy transfer
- gene expression
- mass spectrometry
- drug discovery
- climate change
- metal organic framework
- radiation induced
- rectal cancer