18F-Glyco-RGD Peptides for PET Imaging of Integrin Expression: Efficient Radiosynthesis by Click Chemistry and Modulation of Biodistribution by Glycosylation

2013 ◽  
Vol 11 (2) ◽  
pp. 505-515 ◽  
Author(s):  
Simone Maschauer ◽  
Roland Haubner ◽  
Torsten Kuwert ◽  
Olaf Prante
Keyword(s):  
Click Chemistry ◽  
Pet Imaging ◽  
Integrin Expression ◽  
Rgd Peptides

scholarly journals PET imaging of αvβ3 integrin expression in tumours with 68Ga-labelled mono-, di- and tetrameric RGD peptides

2010 ◽  
Vol 38 (1) ◽  
pp. 128-137 ◽  
Author(s):  
Ingrid Dijkgraaf ◽  
Cheng-Bin Yim ◽  
Gerben M. Franssen ◽  
Robert C. Schuit ◽  
Gert Luurtsema ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Αvβ3 Integrin ◽  
Integrin Expression ◽  
Rgd Peptides

scholarly journals β-Configured clickable [18F]FDGs as novel 18F-fluoroglycosylation tools for PET

2017 ◽  
Vol 41 (18) ◽  
pp. 10231-10236 ◽  
Author(s):  
M. Elgland ◽  
P. Nordeman ◽  
T. Fyrner ◽  
G. Antoni ◽  
K. Peter R. Nilsson ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Pet Imaging ◽  
Prosthetic Groups

We have developed a chemoselective 18F-fluoroglycosylation method for PET imaging that employ β-configured [18F]FDGs as prosthetic groups for 18F-labeling using CuAAC click chemistry.

A developmental analysis of oligodendroglial integrins in primary cells: changes in alpha v-associated beta subunits during differentiation

Development ◽  
1994 ◽  
Vol 120 (12) ◽  
pp. 3497-3506 ◽  
Author(s):  
R. Milner ◽  
C. Ffrench-Constant
Keyword(s):  
Progenitor Cell ◽  
Beta Subunits ◽  
Integrin Expression ◽  
Primary Cells ◽  
Developmentally Regulated ◽  
Rgd Peptides ◽  
Rational Explanation ◽  
Oligodendrocyte Precursor ◽  
Alpha V Beta 3 ◽  
Developmental Analysis

We have examined the expression of integrins on primary oligodendroglial cells during the differentiation of the proliferative oligodendrocyte precursor (O-2A progenitor) cell to the postmitotic oligodendrocyte. Cells of the oligodendrocyte lineage expressed a limited repertoire of integrins: alpha 6 beta 1 and alpha v integrins including alpha v beta 1, alpha v beta 3 and alpha v beta 5, as well as a potentially novel integrin alpha v beta 80 kDa. Integrin expression was developmentally regulated; during differentiation alpha v beta 1 was reduced and alpha v beta 5 upregulated. These results suggest that laminin and vitronectin are important extracellular matrix ligands for oligodendrocytes, and provide a rational explanation for previous observations that RGD peptides inhibit the expression of myelin-specific genes. They also suggest a simple model by which switching of integrin beta subunits might regulate differentiation. As chimeric beta 1 integrins with a beta 5 cytoplasmic domain support proliferation less well than normal beta 1 integrins (Pasqualini and Hemler (1994), J. Cell Biol. 125, 447–460) the switch from alpha v beta 1 to alpha v beta 5 might play a key instructive role in the cessation of proliferation and subsequent differentiation.

scholarly journals PET Radiopharmaceuticals for Imaging Integrin Expression: Tracers in Clinical Studies and Recent Developments

2014 ◽  
Vol 2014 ◽  
pp. 1-17 ◽  
Author(s):  
Roland Haubner ◽  
Simone Maschauer ◽  
Olaf Prante
Keyword(s):  
Nuclear Medicine ◽  
First Generation ◽  
Integrin Expression ◽  
Rgd Peptides ◽  
Recent Developments ◽  
Interesting Approach ◽  
Complex Chemistry ◽  
Pet Radiopharmaceuticals

Noninvasive determination of integrin expression has become an interesting approach in nuclear medicine. Since the discovery of the first18F-labeled cyclic RGD peptide as radiotracer for imaging integrinαvβ3expression in vivo, there have been carried out enormous efforts to develop RGD peptides for PET imaging. Moreover, in recent years, additional integrins, includingα5β1andαvβ6, came into the focus of pharmaceutical radiochemistry. This review will discuss the tracers already evaluated in clinical trials and summarize the preliminary outcome. It will also give an overview on recent developments to further optimize the first-generation compounds such as [18F]Galacto-RGD. This includes recently developed18F-labeling strategies and also new approaches in68Ga-complex chemistry. Furthermore, the approaches to develop radiopharmaceuticals targeting integrinα5β1andαvβ6will be summarized and discussed.

Design, Synthesis, and Evaluation of a Low-Molecular-Weight 11C-Labeled Tetrazine for Pretargeted PET Imaging Applying Bioorthogonal in Vivo Click Chemistry

2016 ◽  
Vol 27 (7) ◽  
pp. 1707-1712 ◽  
Author(s):  
Christoph Denk ◽  
Dennis Svatunek ◽  
Severin Mairinger ◽  
Johann Stanek ◽  
Thomas Filip ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Click Chemistry ◽  
Pet Imaging ◽  
Low Molecular Weight ◽  
Design Synthesis

scholarly journals Click Chemistry for18F-Labeling of RGD Peptides and microPET Imaging of Tumor Integrin αvβ3Expression

2007 ◽  
Vol 18 (6) ◽  
pp. 1987-1994 ◽  
Author(s):  
Zi-Bo Li ◽  
Zhanhong Wu ◽  
Kai Chen ◽  
Frederick T. Chin ◽  
Xiaoyuan Chen
Keyword(s):  
Click Chemistry ◽  
Rgd Peptides ◽  
Micropet Imaging

11C Click Chemistry Using [11C]Methyl Azide: Simplified, Versatile, and Practical Alternative Access to [11C]Nucleosides and [11C]Oligonucleotides for PET Imaging

2013 ◽  
Vol 2013 (7) ◽  
pp. 1214-1217 ◽  
Author(s):  
Thomas Bordenave ◽  
Puja Panwar Hazari ◽  
Damien James ◽  
Anil K. Mishra ◽  
Magali Szlosek-Pinaud ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Pet Imaging
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