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... 

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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…

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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…

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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...

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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…

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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…

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