Cationic eluate pretreatment for automated synthesis of [68Ga]CPCR4.2
09.10.2013
Fostered by the clinical success of sst-ligands, the development and evaluation of 68Ga-labeled peptides have become a very active field in radiopharmaceutical chemistry. Consequently, various new peptide tracers have been developed, e.g. [68Ga]CPCR4.2 for in vivo imaging of solid and haematological tumors or [68Ga]TRAP(RGD)3 for imaging of αvβ3 integrin expression. As a consequence of different matrices (TiO2, SnO2, polymers) exploited in...
PET of CXCR4 expression by a (68)Ga-labeled highly specific targeted contrast agent
01.11.2012
The overexpression of the chemokine receptor CXCR4 plays an important role in oncology, since together with its endogenous ligand, the stromal cell-derived factor (SDF1-α), CXCR4 is involved in tumor development, growth, and organ-specific metastasis. As part of our ongoing efforts to develop highly specific CXCR4-targeted imaging probes and with the aim to assess the suitability of this ligand for first proof-of-concept studies in humans, we further evaluated…
A conformationally frozen peptoid boosts CXCR4 affinity and anti-HIV activity
03.07.2012
There can be only one: Using a peptoid motif obtained by shifting the arginine side chain of a pentapeptide previously developed by Fujii et al. to the neighboring nitrogen atom restricts the conformational freedom…
Design, synthesis, and functionalization of dimeric peptides targeting chemokine receptor CXCR4
12.09.2011
The chemokine receptor CXCR4 is a critical regulator of inflammation and immune surveillance, and it is specifically implicated in cancer metastasis and HIV-1 infection. On the basis of the observation that several of the known antagonists remarkably share a C(2) symmetry element, we constructed symmetric dimers with excellent antagonistic activity using a derivative of a cyclic pentapeptide as monomer. To optimize the binding affinity, we investigated...
PET imaging of CXCR4 receptors in cancer by a new optimized ligand
20.07.2011
The chemokine receptor CXCR4 is a critical regulator of inflammation and immune surveillance, and it is specifically implicated in cancer metastasis and HIV-1 infection. On the basis of the observation that several of the known antagonists remarkably share a C(2) symmetry element, we constructed symmetric dimers with excellent antagonistic activity using a derivative of a cyclic pentapeptide as monomer. To optimize the binding affinity, we investigated…
Introduction of functional groups into peptides via N-alkylation
12.04.2008
An optimized protocol for the mild and selective Fukuyama-Mitsunobu reaction was used for mono- and di- N-alkylation on solid support. Thereby, nonfunctionalized aliphatic and aromatic residues are quickly introduced into transiently protected, primary amines of a linear peptide. N-Alkylation can also be used to implement alkyl chains carrying (protected) functionalities…