
Docking for EP4R antagonists active against inflammatory pain
2023年12月6日 · In this work, seeking to diversify EP4R antagonist scaffolds, we computationally dock over 400 million compounds against an EP4R crystal structure and experimentally …
案例研究 | 分子对接发现 EP4R 拮抗剂在抗炎镇痛的潜力 - 知乎
研究者通过 分子对接 和实验验证,发现了一种高效抗炎的 EP4R 拮抗剂。 本研究使用 EP4R 的晶体结构,通过分子对接筛选超过 4 亿种化合物。 对排名靠前的 71 新合成分子进行实验验证。 …
E-type prostanoid receptor 4 (EP4) in disease and therapy
In this review, we summarize the physiological roles of EP4, its molecular structure and intracellular signaling pathways, and how EP4 receptors might be targeted pharmacologically …
Grapiprant: an EP4 prostaglandin receptor antagonist and novel therapy ...
Grapiprant is a targeted approach to pain management – it selectively blocks the EP4 receptor, does not interfere with the production of prostanoids, and therefore does not affect the other …
E-type prostanoid receptor 4 (EP4) in disease and therapy
A possible explanation for the diverse biological functions of EP4 might be the multiple signaling pathways switched on upon EP4 activation. The present review attempts to summarize the …
A novel prostaglandin E receptor 4 (EP4) small molecule …
2022年3月8日 · Importantly, knocking out EP4 in cartilage enhanced stable mature articular cartilage formation instead of fibrocartilage, and reduced joint pain. In addition, we identified a …
Ligand binding to human prostaglandin E receptor EP4 at the …
2018年12月3日 · Prostaglandin E receptor EP4, a G-protein-coupled receptor, is involved in disorders such as cancer and autoimmune disease. Here, we report the crystal structure of …
Prostaglandin E2 receptor EP4 contributes to inflammatory pain ...
Prostaglandin E(2) (PGE(2)) is both an inflammatory mediator released at the site of tissue inflammation and a neuromodulator that alters neuronal excitability and synaptic processing. …
The prostanoid EP4 receptor and its signaling pathway
2013年6月17日 · The EP4 prostanoid receptor is one of four receptor subtypes for prostaglandin E2. It belongs to the family of G protein-coupled receptors. It was originally identified, similar to …
Discovery of Novel, Selective Prostaglandin EP4 Receptor …
Prostaglandin E2 (PGE 2) receptor 4 (EP4) is one of four EP receptors commonly upregulated in the tumor microenvironment and plays vital roles in stimulating cell proliferation, invasion, and …