Prostaglandin E2 Receptor 4 (EP4): A Promising Therapeutic Target for the Treatment of Cancer and Inflammatory Diseases

Debasis Das, Jiann-Ruey Hong
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引用次数: 5

Abstract

Prostaglandin E2 (PGE2) is involved in several biological processes, including inflammation, pain, fever, renal function, mucosal integrity, angiogenesis and tumor growth. PGE2 receptor subtypes (EP1-4) play pivotal roles in PGE2-mediated biological events. Recent studies revealed the fact that EP4 is commonly upregulated in cancer to stimulate cell proliferation, migration, invasion, and metastasis. Additionally, the EP4 receptor has a role in several anti-inflammatory processes, bone formation and hemostasis. EP4 receptor modulators can be used as drugs of specific interest. A number of EP4 receptor agonists and antagonists are at different stages of clinical development. The agonists of EP4 receptor showed promising results for ulcerative colitis (UC), bone deposition and facilitated bone resorption. The uses of EP4 antagonists, particularly in combination with chemotherapy, endocrine therapy, or immune-based therapies, may be the treatment options for cancer. Several EP4 antagonists are being progressed in clinical trials and hopefully, the results will show the usefulness of EP4 receptor as a target for cancer therapeutics. In this review, we have summarized the EP4 receptor and the possible therapeutic applications of EP4 receptor- selective agonists and antagonists.
前列腺素E2受体4 (EP4):治疗癌症和炎症性疾病的一个有前景的治疗靶点
前列腺素E2 (PGE2)参与多种生物过程,包括炎症、疼痛、发热、肾功能、粘膜完整性、血管生成和肿瘤生长。PGE2受体亚型(EP1-4)在PGE2介导的生物事件中起关键作用。最近的研究表明,EP4在癌症中普遍上调,以刺激细胞增殖、迁移、侵袭和转移。此外,EP4受体在几个抗炎过程、骨形成和止血中发挥作用。EP4受体调节剂可作为特异性药物使用。许多EP4受体激动剂和拮抗剂处于临床开发的不同阶段。ep4受体激动剂在溃疡性结肠炎(UC)、骨沉积和促进骨吸收方面显示出良好的效果。EP4拮抗剂的使用,特别是与化疗、内分泌治疗或免疫治疗联合使用,可能是癌症的治疗选择。几种EP4拮抗剂正在临床试验中进行,希望结果将显示EP4受体作为癌症治疗靶点的有效性。本文综述了EP4受体以及EP4受体选择性激动剂和拮抗剂可能的治疗应用。
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来源期刊
Current Chemical Biology
Current Chemical Biology Medicine-Biochemistry (medical)
CiteScore
1.40
自引率
0.00%
发文量
16
期刊介绍: Current Chemical Biology aims to publish full-length and mini reviews on exciting new developments at the chemistry-biology interface, covering topics relating to Chemical Synthesis, Science at Chemistry-Biology Interface and Chemical Mechanisms of Biological Systems. Current Chemical Biology covers the following areas: Chemical Synthesis (Syntheses of biologically important macromolecules including proteins, polypeptides, oligonucleotides, oligosaccharides etc.; Asymmetric synthesis; Combinatorial synthesis; Diversity-oriented synthesis; Template-directed synthesis; Biomimetic synthesis; Solid phase biomolecular synthesis; Synthesis of small biomolecules: amino acids, peptides, lipids, carbohydrates and nucleosides; and Natural product synthesis).
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