Recent advancements in 18F-labeled PSMA targeting PET radiopharmaceuticals

Two Novel PET Radiopharmaceuticals for Endothelial Vascular Cell Adhesion Molecule-1 (VCAM-1) Targeting

Pharmaceutics ◽

10.3390/pharmaceutics13071025 ◽

2021 ◽

Vol 13 (7) ◽

pp. 1025

Author(s):

Sara Pastorino ◽

Sara Baldassari ◽

Giorgia Ailuno ◽

Guendalina Zuccari ◽

Giuliana Drava ◽

...

Keyword(s):

Cell Adhesion ◽

Adhesion Molecule ◽

Cell Adhesion Molecule ◽

Umbilical Vein ◽

In Vitro Tests ◽

Vascular Cell Adhesion ◽

Vascular Cell ◽

Vascular Cell Adhesion Molecule ◽

Cell Adhesion Molecule 1 ◽

Pet Radiopharmaceuticals

Atherosclerosis is a chronic progressive disease involving inflammatory events, such as the overexpression of adhesion molecules including the endothelial Vascular Cell Adhesion Molecule-1 (VCAM-1). VCAM-1 is rapidly overexpressed in the first stages of atherosclerosis, thus representing a promising target for early atheroma detection. Two novel Positron Emission Tomography (PET) radiopharmaceuticals (MacroP and NAMP), based on the VCAM-1-binding peptide having sequence VHPKQHRGGSKGC, were synthesized and characterized. MacroP is derived from the direct conjugation of a DOTA derivative with the peptide, while NAMP is a biotin derivative conceived to be employed in a three-step pretargeting system, involving the use of a double-chelating derivative of DOTA. The identity of the newly synthesized radiopharmaceuticals was confirmed by mass spectrometry and, after radiolabeling with 68Ga, both showed high radiochemical purity; in vitro tests on human umbilical vein endothelial cells evidenced their VCAM-1 binding ability, with higher radioactive uptake in the case of NAMP. Moreover, NAMP might also be employed in a theranostic approach in association with functionalized biotinylated nanoparticles.

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Rapid and efficient synthesis of [18F]fluoronicotinamides, [18F]fluoroisonicotinamides and [18F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging

Journal of Labelled Compounds and Radiopharmaceuticals ◽

10.1002/jlcr.1869 ◽

2011 ◽

Vol 54 (6) ◽

pp. 312-317 ◽

Cited By ~ 4

Author(s):

I. Al Jammaz ◽

B. Al-Otaibi ◽

S. Okarvi ◽

J. Amartey

Keyword(s):

Efficient Synthesis ◽

Pet Radiopharmaceuticals

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Synthesis and Binding Affinity of Fluorine Containing NG-acyl and -sulfonyl BIBP3226 Derivatives: Ligands for the NPY Y1 Receptor

Australian Journal of Chemistry ◽

10.1071/ch15569 ◽

2016 ◽

Vol 69 (7) ◽

pp. 746

Author(s):

Nigel A. Lengkeek ◽

Maxine P. Roberts ◽

Lei Zhang ◽

I-Chieh J. Lee ◽

Christopher J. R. Fookes ◽

...

Keyword(s):

Binding Affinity ◽

Emission Tomography ◽

Tumour Imaging ◽

Y1 Receptor ◽

Important Amino Acid ◽

Positron Emission ◽

Npy Receptor ◽

Almost All ◽

Derivatives Of ◽

Pet Radiopharmaceuticals

The neuropeptide Y (NPY) receptors are abundant in a range of tumours hence are a molecular target for tumour imaging and therapy, particularly by the use of radiolabelled molecules. NG-Substituted derivatives of the NPY receptor antagonist, BIBP3226, were prepared aiming to improve its current usability and to incorporate a positron-emitting radioisotope for development in positron emission tomography (PET) radiopharmaceuticals. The BIBP3226 derivatives were prepared in seven steps while retaining the critically important amino acid chirality. The acyl derivative retained acceptable ligand binding, however the sulfonyl derivatives lost almost all binding affinity.

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