Prokineticin GPCR Assays
Background of Prokineticins Receptors (PKRs)
Prokineticins are a class of small secreted peptides, including two types: prokineticin-1 and prokineticin-2. They have been proven to exert a wide spectrum of physiological functions by binding to two specific receptors: PKR1 (PK1) and PKR2 (PK2). PKRs are involved in a variety of a wide range of biological activities, including immune responses, metabolism, pain perception, hematopoiesis, and angiogenesis.
Fig.1 Schematic representation of the inflammatory state. (Lattanzi, 2021)
Distribution and Functions of PKRs
PKRs are distributed in a variety of human tissues. PKR1 is discovered mainly in peripheral tissues, such as the neuroendocrine system, reproductive organs, gastrointestinal tract, lung, heart, and macrophages. PKR2 is widely expressed in several organs such as the thyroid, testis, and ovary. Furthermore, PKRs are closely related to the occurrence of various diseases such as gastrointestinal inflammation, obesity, diabetes, multiple sclerosis, stroke, colon cancer, multiple sclerosis, and congenital diseases.
Mechanisms of PKRs
The PKRs are Gq-coupled receptors but may also couple Gi and Gs proteins, suggesting that different pathways participate in prokineticin signaling.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| PKR1 | PROKR1 |
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| PKR2 | PROKR2 |
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Assay List of Prokineticin Receptors
Creative Biolabs can provide a range of assays of prokineticin receptors. You can choose the assay in the list or contact us for more information:
| Assay No. | Assay Name | Host Cell | Assay Type | Datasheet |
|---|---|---|---|---|
| Radioligand Binding Assay | ||||
| S01YF-1122-KX814 | Magic™ Human PROKR1 In Vitro Radioligand Binding Assay | CHO-K1 | Radioligand Binding Assay | |
Published Data
| Paper Title |
PK2β ligand, a splice variant of prokineticin 2, is able to modulate and drive signaling through PKR1 receptor |
| Journal |
Neuropeptides |
| Published | 2018 |
| Abstract |
PK2, a secreted bioactive peptide signaling through PKRs, is involved in the regulation of a variety of biological processes, including nociception, immunity, and angiogenesis. The PK2 primary transcript involves two alternative splicing variants, PK2 and PK2L, that are cleaved into an active peptide called PK2β. Evidence suggested that PK2β preferentially bound to the PKR1 receptor. Using different strains of S. cerevisiae, the researchers characterized PK2β and examined the specificity of PKR1 and PKR2 G-protein coupling after PK2β binding. |
| Result |
This article demonstrated for the first time that PK2β bound preferentially to PKR1, activating a signaling cascade that is independent of Gαi/o coupling. In cells transfected with PKR1 or PKR2, PK2β preferentially binds PKR1 and regulates cAMP accumulation and calcium mobilization via Gαs and Gαq coupling, respectively. In addition, the binding specificity of PK2β to PKR1 was assessed by the analysis of PKR mutants in yeast and glutathione S-transferase (GST) pull-down experiments, revealing the indispensable role of the amino-terminal region of PKR1. The ability of PK2β to differentially activate PKR1 and PKR2 was also assessed by in vivo nociceptive experiments, and the results showed that PK2β induced a strong sensitivity of peripheral nociceptors to painful stimuli via activation of PKR1.
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Fig.2 PK2β preferentially activates PKR1 by Gαq, Gα. (Lattanzi, 2018)
References
- Lattanzi, R.; Miele, R. Versatile Role of Prokineticins and Prokineticin Receptors in Neuroinflammation. Biomedicines. 2021; 9(11): 1648.
- Lattanzi, R.; et al. PK2β ligand, a splice variant of prokineticin 2, is able to modulate and drive signaling through PKR1 receptor. Neuropeptides. 2018; 71: 32-42.
