scholarly journals Radiofluorination of a Pre-formed Gallium(III) Aza-macrocyclic Complex: Towards Next-Generation Positron Emission Tomography (PET) Imaging Agents

2015 ◽  
Vol 21 (12) ◽  
pp. 4688-4694 ◽  
Author(s):  
Rajiv Bhalla ◽  
William Levason ◽  
Sajinder K. Luthra ◽  
Graeme McRobbie ◽  
George Sanderson ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Pet Imaging ◽  
Macrocyclic Complex ◽  
Emission Tomography ◽  
Imaging Agents ◽  
Next Generation ◽  
Positron Emission

scholarly journals Identification, Characterization, and Optimization of Integrin αvβ6-Targeting Peptides from a One-Bead One-Compound (OBOC) Library: Towards the Development of Positron Emission Tomography (PET) Imaging Agents

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 309 ◽  
Author(s):  
Yng Tang ◽  
Ryan Davis ◽  
Tanushree Ganguly ◽  
Julie Sutcliffe
Keyword(s):  
Positron Emission Tomography ◽  
Binding Affinity ◽  
Pet Imaging ◽  
Emission Tomography ◽  
Imaging Agents ◽  
Screening Assay ◽  
Positron Emission ◽  
Integrin Αvβ6 ◽  
Peptide Imaging ◽  
The One

The current translation of peptides identified through the one-bead one-compound (OBOC) technology into positron emission tomography (PET) imaging agents is a slow process, with a major delay between ligand identification and subsequent lead optimization. This work aims to streamline the development process of 18F-peptide based PET imaging agents to target the integrin αvβ6. By directly identify αvβ6–targeting peptides from a 9-mer 4-fluorobenzoyl peptide library using the on-bead two-color (OBTC) cell-screening assay, a total of 185 peptide beads were identified and 5 beads sequenced for further evaluation. The lead peptide 1 (VGDLTYLKK(FB), IC50 = 0.45 ± 0.06 μM, 25% stable in serum at 1 h) was further modified at the N-, C-, and bi-termini. C-terminal PEGylation increased the metabolic stability (>95% stable), but decreased binding affinity (IC50 = 3.7 ± 1 μM) was noted. C-terminal extension (1i, VGDLTYLKK(FB)KVART) significantly increased binding affinity for integrin αvβ6 (IC50 = 0.021 ± 0.002 μM), binding selectivity for αvβ6-expressing cells (3.1 ± 0.8:1), and the serum stability (>99% stable). Our results demonstrate the challenges in optimizing OBOC-derived peptides, indicate both termini of 1 are sensitive to modifications, and show that further modification of 1 is necessary to demonstrate utility as an 18F-peptide imaging agent.

scholarly journals Pyrazoles as Key Scaffolds for the Development of Fluorine-18-Labeled Radiotracers for Positron Emission Tomography (PET)

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1722 ◽  
Author(s):  
Pedro M. O. Gomes ◽  
Artur M. S. Silva ◽  
Vera L. M. Silva
Keyword(s):  
Positron Emission Tomography ◽  
Pet Imaging ◽  
Research Area ◽  
Imaging Systems ◽  
Emission Tomography ◽  
Response To Treatment ◽  
Imaging Agents ◽  
Chemical Probes ◽  
Medical Treatments ◽  
Positron Emission

The need for increasingly personalized medicine solutions (precision medicine) and quality medical treatments, has led to a growing demand and research for image-guided therapeutic solutions. Positron emission tomography (PET) is a powerful imaging technique that can be established using complementary imaging systems and selective imaging agents—chemical probes or radiotracers—which are drugs labeled with a radionuclide, also called radiopharmaceuticals. PET has two complementary purposes: selective imaging for diagnosis and monitoring of disease progression and response to treatment. The development of selective imaging agents is a growing research area, with a high number of diverse drugs, labeled with different radionuclides, being reported nowadays. This review article is focused on the use of pyrazoles as suitable scaffolds for the development of 18F-labeled radiotracers for PET imaging. A brief introduction to PET and pyrazoles, as key scaffolds in medicinal chemistry, is presented, followed by a description of the most important [18F]pyrazole-derived radiotracers (PET tracers) that have been developed in the last 20 years for selective PET imaging, grouped according to their specific targets.

scholarly journals Synthesis of novel neutrophil-specific imaging agents for Positron Emission Tomography (PET) imaging

2007 ◽  
Vol 17 (24) ◽  
pp. 6876-6878 ◽  
Author(s):  
Yi Zhang ◽  
Bijoy Kundu ◽  
Karen D. Fairchild ◽  
Landon Locke ◽  
Stuart S. Berr ◽  
...  
Keyword(s):  
Positron Emission Tomography ◽  
Pet Imaging ◽  
Emission Tomography ◽  
Imaging Agents ◽  
Positron Emission
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