Synthesis and characterization of [125I]TZ6544, a promising radioligand for investigating sphingosine-1-phosphate receptor 2

Luo, Zonghua; Liang, Qianwa; Liu, Hui; Joshi, Sumit; Jiang, Hao; Klein, Robyn S.

doi:10.1016/j.nucmedbio.2020.07.007

Cited by 3 publications

(3 citation statements)

References 36 publications

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“…This section will provide a comprehensive compendium of the rational design of S1PR2 modulators. 98 The scaffold hopping strategies were carried out based on the structures of sphingosine or S1P to get better S1PR agonists. Fingolimod (2, FTY720) is a prodrug and can be phosphorylated to FTY720 (S)-phosphate (3, FTY720-P) by Sphk2 in vivo, 99 which then stimulates S1P receptors (Figure 10C).…”

Section: S1pr2 Modulatorsmentioning

confidence: 99%

An overview of sphingosine‐1‐phosphate receptor 2: Structure, biological function, and small‐molecule modulators

Hao,

Luo,

Jiang

et al. 2024

Medicinal Research Reviews

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Over the past decade, there has been a notable increase in research on sphingosine‐1‐phosphate receptor 2 (S1PR2), which is a type of G‐protein‐coupled receptor. Upon activation by S1P or other ligands, S1PR2 initiates downstream signaling pathways such as phosphoinositide 3‐kinase (PI3K), Mitogen‐activated protein kinase (MAPK), Rho/Rho‐associated coiled‐coil containing kinases (ROCK), and others, contributing to the diverse biological functions of S1PR2 and playing a pivotal role in various physiological processes and disease progressions, such as multiple sclerosis, fibrosis, inflammation, and tumors. Due to the extensive biological functions of S1PR2, many S1PR2 modulators, including agonists and antagonists, have been developed and discovered by pharmaceutical companies (e.g., Novartis and Galapagos NV) and academic medicinal chemists for disease diagnosis and treatment. However, few reviews have been published that comprehensively overview the functions and regulators of S1PR2. Herein, we provide an in‐depth review of the advances in the function of S1PR2 and its modulators. We first summarize the structure and biological function of S1PR2 and its pathological role in human diseases. We then focus on the discovery approach, design strategy, development process, and biomedical application of S1PR2 modulators. Additionally, we outline the major challenges and future directions in this field. Our comprehensive review will aid in the discovery and development of more effective and clinically applicable S1PR2 modulators.

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Section: S1pr2 Modulatorsmentioning

confidence: 99%

An overview of sphingosine‐1‐phosphate receptor 2: Structure, biological function, and small‐molecule modulators

Hao,

Luo,

Jiang

et al. 2024

Medicinal Research Reviews

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“…Most recently, a 125 I-labeled ligand [ 123 I]79 ([ 123 I]TZ6544) was disclosed with excellent binding affinity (K d = 4.31 nM), high selectivity (>300-fold over S1PR1, S1PR3, S1PR4, and S1PR5), and binding specificity toward S1PR2. 266…”

Section: Pet Probes For Sphingosine-1-phosphatementioning

confidence: 99%

“… Despite limited brain uptake in mice due to an interaction with P-gp, [ 11 C]TZ34125 was sensitive to sexual dimorphism of S1PR2 expression in SJL mice (SUV = 0.58 and 0.48, respectively, in female and male mouse cerebellum at 30 min p.i.). Most recently, a 125 I-labeled ligand [ 123 I] 79 ([ 123 I]TZ6544) was disclosed with excellent binding affinity ( K d = 4.31 nM), high selectivity (>300-fold over S1PR1, S1PR3, S1PR4, and S1PR5), and binding specificity toward S1PR2 …”

Section: Pet Probes For Sphingosine-1-phosphate Receptor (S1pr)mentioning

confidence: 99%

The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO

et al. 2021

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Neuroinflammation is an adaptive response of the central nervous system to diverse potentially injurious stimuli, which is closely associated with neurodegeneration and typically characterized by activation of microglia and astrocytes. As a noninvasive and translational molecular imaging tool, positron emission tomography (PET) could provide a better understanding of neuroinflammation and its role in neurodegenerative diseases. Ligands to translator protein (TSPO), a putative marker of neuroinflammation, have been the most commonly studied in this context, but they suffer from serious limitations. Herein we present a repertoire of different structural chemotypes and novel PET ligand design for classical and emerging neuroinflammatory targets beyond TSPO. We believe that this Perspective will support multidisciplinary collaborations in academic and industrial institutions working on neuroinflammation and facilitate the progress of neuroinflammation PET probe development for clinical use.

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Naturally occurring delta-9-tetrahydrocannabinol derivatives and binding to CB1 and CB2 receptors: Linking in the endocannabinoid system

Reyes‐Resina

Rivas‐Santisteban

Raïch

et al. 2023

Neurobiology and Physiology of the Endocannabinoid System

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Synthesis and characterization of [125I]TZ6544, a promising radioligand for investigating sphingosine-1-phosphate receptor 2

Cited by 3 publications

References 36 publications

An overview of sphingosine‐1‐phosphate receptor 2: Structure, biological function, and small‐molecule modulators

An overview of sphingosine‐1‐phosphate receptor 2: Structure, biological function, and small‐molecule modulators

The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO

Naturally occurring delta-9-tetrahydrocannabinol derivatives and binding to CB1 and CB2 receptors: Linking in the endocannabinoid system

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