The present disclosure relates to a compound and pharmaceutically mPGES-1 inhibitors of formula (I) acceptable salt thereof. 这些化合物是微粒体前列腺素E合酶1(mPGES1)酶的抑制剂,且因此可用于治疗由多种疾病或病症(诸如哮喘,骨关节炎,类风湿性关节炎,急性或慢性疼痛和神经变性疾病)引起的疼痛和/或炎症....
and various inhibitors have been reported in the literature. However, none of the reported potent inhibitors of human mPGES-1 has shown to be also a potent inhibitor of mouse or rat mPGES-1, which prevents using
目的:总结COX-2和mPGEs-1的生物学作用以及肿瘤的研究进展,探讨COX-2和mPGEs-1选择性抑制剂在肿瘤治疗中的作用,为癌症的临床治疗提供参考.方法:利用PubMed数据库检索系统,以"COX-2、mPGEs-1、肿瘤"为关键词,检索到相关文献785篇,排除与本研究无关的文献,再将COX-2、mPGEs-1的生物学作用、COX-2和mPGEs-1选择...
Transcriptional Regulation of mPGES1 in Cancer: An Alternative Approach to Drug Discovery?CancerinflammationinhibitorsprostaglandinEsynthasetranscriptionfactorsProstaglandins serve as the connecting link between inflammation and cancer. mPGES1, the downstream enzyme in the prostaglandin pathway is considered a ...
Microsomal (m) PGE synthase (S)-1, the dominant synthetic enzyme for PGE2production in vivo5, is being considered as a new therapeutic target downstream of COX6,7,8. In contrast to COX-2 inhibitors, deletion ofmPges-1augments PGI2production, restraining thrombogenesis and atherogenesis, and mo...
The invention further is related to identifying inhibitors of mPGES-1 that do not increase cardiovascular risk when administered to an individual. 二、法律状态 暂无信息 三、权利要求 暂无信息 四、说明书暂无信息 打开APP,查看更多专利的权利要求、说明书...
identified in the 1 h to 3 h comparison, in the regulation of TNFα-induced mPGES-1 and COX-2 expression. For this purpose, we investigated the effect of specific inhibitors of the JNK and NF-κB signal pathways on the expression of mPGES-1 and COX-2 as well as on the phosphorylation...
identified in the 1 h to 3 h comparison, in the regulation of TNFα-induced mPGES-1 and COX-2 expression. For this purpose, we investigated the effect of specific inhibitors of the JNK and NF-κB signal pathways on the expression of mPGES-1 and COX-2 as well as on the phosphorylation...
The competitive inhibitors, in particular, may interact with the arachidonic acid binding pocket or with a putative allosteric site [101]. Considering the chemical nature of TIIA and CRY, it can be hypothesized that these may act as “canonical” competitive inhibitors (i.e., that interfere ...
Computational models for the classification of mPGES-1 inhibitors with fingerprint descriptorsMicrosomal prostaglandinE2\\documentclass[12pt]{minimal} \\usepackage{amsmath} \\usepackage{wasysym} \\usepackage{amsfonts} \\usepackage{amssymb} \\usepackage{amsbsy} \\usepackage{mathrsfs} \\usepackage{up...