Experimental Research Progress of mPGES-1 Inhibitor 2,5- dimethylcelecoxib in Various Diseases.

IF 3.5 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Current medicinal chemistry Pub Date : 2026-01-01 DOI:10.2174/0109298673327820241004042817
Zhanfei Chen, Rong Chen, Laiping Wang, Zihao Yu, Weitong Chen, Hua Lin, Liumin Yu, Jinqiu Li, Zhonghui Chen, Jianlin Shen, Nanhong Tang
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Abstract

Prostaglandin E2 (PGE2) plays a crucial role in inflammation. Non-steroidal anti-inflammatory medications are commonly utilized to alleviate pain and address inflammation by blocking the production of PGE2 and cyclooxygenase (COX). However, selective inhibition of COX can easily lead to a series of risks for cardiovascular diseases. Hence, it is imperative to discover safer and more efficient targets for reducing inflammation. Research has demonstrated that mPGES-1 serves as the final enzyme that controls the rate of prostaglandin E2 synthesis. Moreover, it is only triggered by inflammation and could serve as a possible treatment target instead of COX in cases of inflammation. 2,5-dimethylcelecoxib (DMC) can effectively inhibit mPGES-1 expression, maintain the overall balance of prostaglandins, reduce the secretion of PGE2, and, most importantly, avoid the side effects of COX inhibitors. DMC has the ability to address illnesses through the stimulation of autophagy and apoptosis, as well as the regulation of the immune microenvironment and intestinal flora. This study provides a comprehensive overview of the advancements in DMC within experimental research and offers suggestions for potential avenues of future investigation.

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mPGES-1抑制剂2,5-二甲基塞来昔布在多种疾病中的实验研究进展
前列腺素E2 (PGE2)在炎症中起着关键作用。非甾体类抗炎药物通常通过阻断PGE2和环氧合酶(COX)的产生来缓解疼痛和解决炎症。然而,COX的选择性抑制容易导致一系列心血管疾病的风险。因此,发现更安全、更有效的消炎靶点势在必行。研究表明,mPGES-1是控制前列腺素E2合成速率的最终酶。此外,它仅由炎症触发,在炎症情况下可以代替COX作为可能的治疗靶点。2,5-二甲基塞来昔布(DMC)可以有效抑制mPGES-1的表达,维持前列腺素的整体平衡,减少PGE2的分泌,最重要的是避免COX抑制剂的副作用。DMC具有通过刺激自噬和细胞凋亡,以及调节免疫微环境和肠道菌群来治疗疾病的能力。本研究综述了DMC在实验研究中的进展,并对未来的研究方向提出了建议。
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来源期刊
Current medicinal chemistry
Current medicinal chemistry 医学-生化与分子生物学
CiteScore
8.60
自引率
2.40%
发文量
468
审稿时长
3 months
期刊介绍: Aims & Scope Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews and guest edited thematic issues written by leaders in the field covering a range of the current topics in medicinal chemistry. The journal also publishes reviews on recent patents. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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