Targeting EP2 Receptor for Drug Discovery: Strengths, Weaknesses, Opportunities, and Threats (SWOT) Analysis.
Targeting EP2 Receptor for Drug Discovery: Strengths, Weaknesses, Opportunities, and Threats (SWOT) Analysis.
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DOI：
10.1021/acs.jmedchem.3c00655
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发表时间：
2023-07-27
影响因子：
7.3
通讯作者：
Ganesh, Thota
中科院分区：
文献类型：
--
作者：
Ganesh, Thota
环氧合酶-1和-2（COX 1和COX 2）衍生的内源性配体前列腺素E2（PGE 2）引发多种生理和病理状况。它通过四种G蛋白偶联受体EP 1、EP 2、EP 3和EP 4介导信号传导。其中，EP 2在包括大脑和子宫在内的整个身体中表达。已经使用EP 2基因敲除小鼠、细胞模型和该受体的选择性小分子激动剂和拮抗剂广泛研究了EP 2的功能作用。来自体外和体内动物模型的功效数据表明，EP 2受体是在多种疾病中具有有害功能的主要促炎介质，这表明EP 2抑制剂作为下一代选择性抗炎和抗增殖剂的前进道路。有趣的是，在某些疾病中，EP 2作用是有益的;因此，EP 2激动剂似乎在临床上有用。在这里，我们强调了针对EP 2受体的优势，劣势，机会和潜在威胁（SWOT分析），用于各种未满足的临床需求的治疗开发。
Cyclooxygenase-1 and -2 (COX1 and COX2) derived endogenous ligand prostaglandin-E2 (PGE2) triggers several physiological and pathological conditions. It mediates signaling through four G-protein coupled receptors, EP1, EP2, EP3, and EP4. Among these, EP2 is expressed throughout the body including the brain and uterus. The functional role of EP2 has been extensively studied using EP2 gene knockout mice, cellular models, and selective small molecule agonists and antagonists for this receptor. The efficacy data from in vitro and in vivo animal models indicate that EP2 receptor is a major proinflammatory mediator with deleterious functions in a variety of diseases suggesting a path forward for EP2 inhibitors as the next generation of selective anti-inflammatory and antiproliferative agents. Interestingly in certain diseases, EP2 action is beneficial; therefore, EP2 agonists seem to be clinically useful. Here, we highlight the strengths, weaknesses, opportunities, and potential threats (SWOT analysis) for targeting EP2 receptor for therapeutic development for a variety of unmet clinical needs.
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影响因子：
6.1
作者：
Jiang, Jianxiong;Yang, Myung-Soon;Quan, Yi;Gueorguieva, Paoula;Ganesh, Thota;Dingledine, Raymond
通讯作者：
Dingledine, Raymond
DOI：
10.1016/j.biopha.2022.112646
发表时间：
2022-03
期刊：
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
影响因子：
--
作者：
Rawat V;Banik A;Amaradhi R;Rojas A;Taval S;Nagy T;Dingledine R;Ganesh T
通讯作者：
Ganesh T
影响因子：
5.4
作者：
Huang M;Weiss WA
通讯作者：
Weiss WA
影响因子：
20.1
作者：
Arehart, Eric;Stitham, Jeremiah;Hwa, John
通讯作者：
Hwa, John
影响因子：
7.3
作者：
Fox, Brian M.;Beck, Hilary P.;Olson, Steven H.
通讯作者：
Olson, Steven H.