Indole-Based and Cyclopentenylindole-Based Analogues Containing Fluorine Group as Potential 18F-Labeled Positron Emission Tomography (PET) G-Protein Coupled Receptor 44 (GPR44) Tracers

Recently, growing evidence of the relationship between G-protein coupled receptor 44 (GPR44) and the inflammation-cancer system has garnered tremendous interest, while the exact role of GPR44 has not been fully elucidated. Currently, there is a strong and urgent need for the development of non-invas...

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Published in:Pharmaceuticals (Basel, Switzerland) Switzerland), 2023-08, Vol.16 (9), p.1203
Main Authors: Yin, Runkai, Huang, Kelly X., Huang, Lina A., Ji, Melinda, Zhao, Hanyi, Li, Kathy, Gao, Anna, Chen, Jiaqi, Li, Zhixuan, Liu, Tianxiong, Shively, John E., Kandeel, Fouad, Li, Junfeng
Format: Article
Language:English
Subjects:
Apoptosis
Asthma
cancer-related inflammation
Carbon
Colorectal cancer
Cytokines
Fluorine
fluorine-18
G-protein coupled receptor 44 (GPR44)
Gastric cancer
indole-based analogues
Inflammation
inflammation-induced cancer
Kinases
Labeling
Lung cancer
Magnetic resonance imaging
Physiology
positron emission tomography (PET) imaging
Proteins
Review
Tomography
Tumor necrosis factor-TNF
Tumors
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Summary:Recently, growing evidence of the relationship between G-protein coupled receptor 44 (GPR44) and the inflammation-cancer system has garnered tremendous interest, while the exact role of GPR44 has not been fully elucidated. Currently, there is a strong and urgent need for the development of non-invasive in vivo GPR44 positron emission tomography (PET) radiotracers that can be used to aid the exploration of the relationship between inflammation and tumor biologic behavior. Accordingly, the choosing and radiolabeling of existing GPR44 antagonists containing a fluorine group could serve as a viable method to accelerate PET tracers development for in vivo imaging to this purpose. The present study aims to evaluate published (2000-present) indole-based and cyclopentenyl-indole-based analogues of the GPR44 antagonist to guide the development of fluorine-18 labeled PET tracers that can accurately detect inflammatory processes. The selected analogues contained a crucial fluorine nuclide and were characterized for various properties including binding affinity, selectivity, and pharmacokinetic and metabolic profile. Overall, 26 compounds with favorable to strong binding properties were identified. This review highlights the potential of GPR44 analogues for the development of PET tracers to study inflammation and cancer development and ultimately guide the development of targeted clinical therapies.
ISSN:1424-8247
1424-8247
DOI:10.3390/ph16091203