Development of a CCR2 targeted 18F-labeled radiotracer for atherosclerosis imaging with PET

Copyright © 2024 Elsevier Inc. All rights reserved..

Atherosclerosis is a chronic inflammatory disease and the leading cause of morbidity and mortality worldwide. CC motif chemokine ligand 2 and its corresponding cognate receptor 2 (CCL2/CCR2) signaling has been implicated in regulating monocyte recruitment and macrophage polarization during inflammatory responses that plays a pivotal role in atherosclerosis initiation and progression. In this study, we report the design and synthesis of a novel 18F radiolabeled small molecule radiotracer for CCR2-targeted positron emission tomography (PET) imaging in atherosclerosis. The binding affinity of this radiotracer to CCR2 was evaluated via in vitro binding assay using CCR2+ membrane and cells. Ex vivo biodistribution was carried out in wild type mice to assess radiotracer pharmacokinetics. CCR2 targeted PET imaging of plaques was performed in two murine atherosclerotic models. The sensitive detection of atherosclerotic lesions highlighted the potential of this radiotracer for CCR2 targeted PET and warranted further optimization.

Medienart:

E-Artikel

Erscheinungsjahr:

2024

Erschienen:

2024

Enthalten in:

Zur Gesamtaufnahme - volume:130-131

Enthalten in:

Nuclear medicine and biology - 130-131(2024) vom: 29. März, Seite 108893

Sprache:

Englisch

Beteiligte Personen:

Zhang, Xiaohui [VerfasserIn]
Qiu, Lin [VerfasserIn]
Sultan, Debbie H [VerfasserIn]
Luehmann, Hannah P [VerfasserIn]
Yu, Yanbo [VerfasserIn]
Zhang, Xiuli [VerfasserIn]
Heo, Gyu Seong [VerfasserIn]
Li, Alexandria [VerfasserIn]
Lahad, Divangana [VerfasserIn]
Rho, Shinji [VerfasserIn]
Tu, Zhude [VerfasserIn]
Liu, Yongjian [VerfasserIn]

Links:

Volltext

Themen:

(18)F radiolabeling
Atherosclerosis
CCR2
Journal Article
Macrophages
PET/CT
Radiopharmaceuticals

Anmerkungen:

Date Completed 25.03.2024

Date Revised 28.03.2024

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1016/j.nucmedbio.2024.108893

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM369128192