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PET imaging of αvβ3 integrin expression in tumours with 68Ga-labelled mono-, di- and tetrameric RGD peptides
- I. Dijkgraaf, C. Yim, O. Boerman
- Chemistry, BiologyEuropean Journal of Nuclear Medicine and…
- 21 September 2010
The αvβ3-binding characteristics of 68Ga-labelled monomeric, dimeric and tetrameric RGD peptides were determined and compared with their 111In-labelling counterparts and the integrin affinity and the tumour uptake followed the order of DOTA-tetramer >DOTA-dimer > Dota-monomer.
PET of EGFR with (64) Cu-cetuximab-F(ab')2 in mice with head and neck squamous cell carcinoma xenografts.
Clinically, this tracer has the potential to be used to determine cetuximab targeting of tumors and possibly to non-invasively monitor the response to EGFR-inhibitor treatment and is a promising PET tracer to determine expression of EGFR in vivo.
64Cu- and 68Ga-labelled [Nle(14),Lys(40)(Ahx-NODAGA)NH2]-exendin-4 for pancreatic beta cell imaging in rats.
- K. Mikkola, C. Yim, P. Nuutila
- Medicine, BiologyMolecular imaging and biology : MIB : the…
- 1 April 2014
Glucagon-like peptide-1 receptor (GLP-1R)-specific labelling of pancreatic islets was found, however, the pancreas could not be visualised in PET images and the highest uptake of the tracers was observed in the kidneys.
‘Sulfo‐click’ for ligation as well as for site‐specific conjugation with peptides, fluorophores, and metal chelators
- D. Rijkers, R. Merkx, C. Yim, A. J. Brouwer, R. Liskamp
- Chemistry, BiologyJournal of peptide science : an official…
- 1 January 2010
Detailed protocols are provided for decorating biologically active peptides or dendrimers with biophysical tags, fluorescent probes, metal chelators, and small peptides by using this reaction as a novel, metal‐free ‘sulfo‐click’ approach.
Synthesis of DOTA-conjugated multimeric [Tyr3]octreotide peptides via a combination of Cu(I)-catalyzed "click" cycloaddition and thio acid/sulfonyl azide "sulfo-click" amidation and their in vivo…
The design, synthesis, and biological evaluation of a series of DOTA-conjugated monomeric, dimeric, and tetrameric [Tyr(3)]octreotide-based analogues as a tool for tumor imaging and/or radionuclide therapy and can be exploited for therapeutic applications are described.
Synthesis and Preclinical Evaluation of Radio-Iodinated GRPR/PSMA Bispecific Heterodimers for the Theranostics Application in Prostate Cancer
The GRPR/PSMA-targeting heterodimer [125I]I-BO530 is a promising agent for theranostics application in prostate cancer.
Versatile conjugation of octreotide to dendrimers by cycloaddition ("click") chemistry to yield high-affinity multivalent cyclic Peptide dendrimers.
The design and synthesis of a series of Tyr(3)-octreotide-containing monomeric, dimeric, and tetrameric dendrimeric conjugates, which have high affinities for the SSTR2 receptor were described and determined by a competitive binding assay on rat brain sections.
Synthesis and preclinical characterization of [64Cu]NODAGA-MAL-exendin-4 with a Nε-maleoyl-L-lysyl-glycine linkage.
Dimeric [68Ga]DOTA-RGD Peptide Targeting αvβ3 Integrin Reveals Extracellular Matrix Alterations after Myocardial Infarction
The results show that integrin-targeting [68Ga]DOTA-E-[c(RGDfK)]2 is a potential tracer for monitoring of myocardial extracellular matrix remodeling after MI using PET.
Low kidney uptake of GLP-1R-targeting, beta cell-specific PET tracer, 18F-labeled [Nle14,Lys40]exendin-4 analog, shows promise for clinical imaging
18F]exendin-4 showed promise as a tracer for clinical imaging of pancreatic β cells, due to its high specific uptake in native β cells and its concomitant low kidney radioactivity uptake.