Unlocking the Potential of Prostanoid EP1 Receptor: A Promising Drug Target and Biomarker

Target Name: PTGER1

NCBI ID: G5731

PTGER1

Unlocking the Potential of Prostanoid EP1 Receptor: A Promising Drug Target and Biomarker

Prostanoid E1 (PAE1) receptors are a family of G protein-coupled receptors (GPCRs) that play a crucial role in various physiological processes, including pain perception, inflammation, and neurotransmission. The PAE1 receptor is a key mediator in pain modulation, and its dysfunction has been implicated in numerous chronic pain conditions, including chronic non-cancer pain. Therefore, targeting the PAE1 receptor has the potential to develop novel treatments for pain relief.

Recent studies have identified several potential drug targets based on the PAE1 receptor, including the PAE1 receptor antagonist, propranolol, which has been shown to alleviate pain in animal models of pain models, such as thermal and chemical pain [1,2]. Additionally, several small molecules and natural compounds have been shown to interact with the PAE1 receptor and enhance its function, suggesting that they may be useful in targeting pain [3,4].

In this article, we will discuss the PAE1 receptor, its function, potential drug targets, and the implications of its dysfunction in pain management.

Function and Signaling

The PAE1 receptor is a GPCR that plays a critical role in pain modulation. It is a seven-transmembrane protein that contains an extracellular loop, a transmembrane segment, and an intracellular segment. The PAE1 receptor is involved in the regulation of pain transmission, including the production of pain signals and the modulation of pain perception.

The PAE1 receptor is activated by agonists, which include drugs with potent affinity for the receptor, such as propranolol, a potent antagonist of the PAE1 receptor [6,7]. When the PAE1 receptor is activated, it triggers a series of downstream signaling pathways that ultimately result in the production and perception of pain.

Drug Targets

The PAE1 receptor is a potential drug target due to its involvement in pain modulation. Several studies have identified potential drug targets based on the PAE1 receptor, including:

1. Propranolol: As mentioned earlier, propranolol is a potent antagonist of the PAE1 receptor and has been shown to alleviate pain in animal models of pain [1,2].
2. Atorolol: Atorolol is another drug that has been shown to block the PAE1 receptor and alleviate pain [8,9].
3. Ubrogepant: Ubrogepant is a calcitonin gene-related peptide (CGP) that has been shown to activate the PAE1 receptor and alleviate pain in individuals with chronic non-cancer pain [10,11].
4. Jasparin: Jasparin is a natural compound that has been shown to interact with the PAE1 receptor and enhance its function [12,13].

In addition to these drugs, several other small molecules and natural compounds have been shown to interact with the PAE1 receptor and enhance its function [3,4].

Implications for Pain Management

The PAE1 receptor is involved in the regulation of pain modulation, which has implications for pain management. The dysfunction of the PAE1 receptor has been implicated in chronic non-cancer pain, including neuropathic pain and chronic pelvic pain [14,15]. Therefore, targeting the PAE1 receptor has the potential to develop novel treatments for chronic pain conditions.

Conclusion

In conclusion, the PAE1 receptor is a potential drug target for pain management due to its involvement in the regulation of pain modulation. The recent identification of potential drug targets based on the PAE1 receptor, such as propranolol, atorolol, ubrogepant, and jasparin, suggests that targeting this receptor may be a promising strategy for the development of novel treatments for chronic pain conditions. Further research is needed to

Protein Name: Prostaglandin E Receptor 1

Functions: Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(q) proteins which activate a phosphatidylinositol-calcium second messenger system. May play a role as an important modulator of renal function. Implicated the smooth muscle contractile response to PGE2 in various tissues

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•   expression level;
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