A Solid-Phase Labeling Strategy for the Preparation of Technetium and Rhenium Bifunctional Chelate Complexes and Associated Peptide Conjugates

2006 ◽  
Vol 17 (1) ◽  
pp. 226-235 ◽  
Author(s):  
R. William Riddoch ◽  
Paul Schaffer ◽  
John F. Valliant
Keyword(s):  
Solid Phase ◽  
Chelate Complexes ◽  
Peptide Conjugates

68Ga-labeled HBED-CC Variant of uPAR Targeting Peptide AE105 Compared with 68Ga-NODAGA-AE105

2019 ◽  
Vol 18 (9) ◽  
pp. 1289-1294 ◽  
Author(s):  
Kusum Vats ◽  
Rohit Sharma ◽  
Haladhar D. Sarma ◽  
Drishty Satpati ◽  
Ashutosh Dash
Keyword(s):  
Solid Phase ◽  
Evaluation Studies ◽  
Radiochemical Yield ◽  
In Vivo Evaluation ◽  
Peptide Conjugates ◽  
Biodistribution Studies ◽  
Target Organs ◽  
U87mg Tumor

Aims: The urokinase Plasminogen Activator Receptors (uPAR) over-expressed on tumor cells and their invasive microenvironment are clinically significant molecular targets for cancer research. uPARexpressing cancerous lesions can be suitably identified and their progression can be monitored with radiolabeled uPAR targeted imaging probes. Hence this study aimed at preparing and evaluating two 68Ga-labeled AE105 peptide conjugates, 68Ga-NODAGA-AE105 and 68Ga-HBED-CC-AE105 as uPAR PET-probes. Method: The peptide conjugates, HBED-CC-AE105-NH2 and NODAGA-AE105-NH2 were manually synthesized by standard Fmoc solid phase strategy and subsequently radiolabeled with 68Ga eluted from a commercial 68Ge/68Ga generator. In vitro cell studies for the two radiotracers were performed with uPAR positive U87MG cells. Biodistribution studies were carried out in mouse xenografts with the subcutaneously induced U87MG tumor. Results: The two radiotracers, 68Ga-NODAGA-AE105 and 68Ga-HBED-CC-AE105 that were prepared in >95% radiochemical yield and >96% radiochemical purity, exhibited excellent in vitro stability. In vivo evaluation studies revealed higher uptake of 68Ga-HBED-CC-AE105 in U87MG tumor as compared to 68Ga-NODAGAAE105; however, increased lipophilicity of 68Ga-HBED-CC-AE105 resulted in slower clearance from blood and other non-target organs. The uPAR specificity of the two radiotracers was ascertained by significant (p<0.05) reduction in the tumor uptake with a co-injected blocking dose of unlabeled AE-105 peptide. Conclusion: Amongst the two radiotracers studied, the neutral 68Ga-NODAGA-AE105 with more hydrophilic chelator exhibited faster clearance from non-target organs. The conjugation of HBED-CC chelator (less hydrophilic) resulted in negatively charged 68Ga-HBED-CC-AE105 which was observed to have high retention in blood that decreased target to non-target ratios.

Synthesis of Peptide-PNA-Peptide Conjugates by Semi-Solid-Phase Chemical Ligation Combined with Deactivation/Capture of Excess Reactants

2004 ◽  
Vol 2004 (4) ◽  
pp. 850-857 ◽  
Author(s):  
Martijn C. de Koning ◽  
Dmitri V. Filippov ◽  
Gijsbert A. van der Marel ◽  
Jacques H. van Boom ◽  
Mark Overhand
Keyword(s):  
Solid Phase ◽  
Peptide Conjugates ◽  
Chemical Ligation ◽  
Semi Solid ◽  
Phase Chemical

An Fmoc solid-phase approach to linear polypyrrole-peptide conjugates

1999 ◽  
Vol 40 (18) ◽  
pp. 3621-3624 ◽  
Author(s):  
Eugenio Vázquez ◽  
Ana M. Caamaño ◽  
Luis Castedo ◽  
JoséL. Mascareñas
Keyword(s):  
Solid Phase ◽  
Peptide Conjugates ◽  
Phase Approach

Facile solid-phase synthesis of PNA–peptide conjugates using pNZ-protected PNA monomers

2014 ◽  
Vol 1 (9) ◽  
pp. 1050-1054 ◽  
Author(s):  
Yi-Chao Huang ◽  
Cheng Cao ◽  
Xiang-Long Tan ◽  
Xiaoyu Li ◽  
Lei Liu
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Peptide Conjugates ◽  
Phase Synthesis

Direct Fmoc/tert-Bu solid phase synthesis of octamannosyl polylysine dendrimer-peptide conjugates

Biopolymers ◽  
2006 ◽  
Vol 84 (2) ◽  
pp. 232-240 ◽  
Author(s):  
Eric Assen B. Kantchev ◽  
Chung-Chieh Chang ◽  
Ding-Kwo Chang
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Peptide Conjugates ◽  
Phase Synthesis

Solid-Phase Synthesis of Peptide Conjugates Derived from the Antimicrobial Cyclic Decapeptide BPC194

2015 ◽  
Vol 2015 (5) ◽  
pp. 1117-1129 ◽  
Author(s):  
Sílvia Vilà ◽  
Esther Badosa ◽  
Emilio Montesinos ◽  
Lidia Feliu ◽  
Marta Planas
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Peptide Conjugates ◽  
Phase Synthesis
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