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The Role of Celecoxib as a Potential Inhibitor in the Treatment of Inflammatory Diseases - A Review.
Current Medicinal Chemistry ( IF 3.5 ) Pub Date : 2022-01-01 , DOI: 10.2174/0929867328666210910125229
Josiane Viana Cruz 1, 2 , Joaquín María Campos Rosa 2, 3, 4 , Njogu Mark Kimani 2, 5 , Silvana Giuliatti 2, 6 , Cleydson Breno Rodrigues Dos Santos 1, 2, 3
Affiliation  

This article aims at reviewing celecoxib as a potential inhibitor in the treatment of inflammatory diseases. The enzyme cyclooxygenase (COX) predominantly has two isoforms called cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2). The former plays a constitutive role related to homeostatic effects in renal and platelets, while the latter is mainly responsible for the induction of inflammatory effects. Since COX-2 plays an important role in the pathogenesis of inflammatory diseases, it has been signaled as a target for the planning of anti-inflammatory intermediates. Many inhibitors developed and planned for COX-2 inhibition have presented side effects to humans, mainly in the gastrointestinal and/or cardiovascular tract. Therefore, it is necessary to design new potential COX-2 inhibitors, which are relatively safe and have no side effects. In this sense, celecoxib is the only potent, selective COX-2 inhibitor that is still commercially available (within the "coxib" family). Thus, celecoxib became a commercial prototype inhibitor for the development of anti-inflammatory agents for the COX-2 enzyme. This review provides inhibition highlights that should provide a structural basis for the design of promising new non-steroidal anti-inflammatory drugs (NSAIDs), which act as COX-2 inhibitors with lesser side effects on the human body.

中文翻译:

塞来昔布作为潜在抑制剂在炎症性疾病治疗中的作用——综述。

本文旨在回顾塞来昔布作为治疗炎症性疾病的潜在抑制剂。酶环氧合酶 (COX) 主要具有两种异构体,称为环氧合酶 1 (COX-1) 和环氧合酶 2 (COX-2)。前者在肾脏和血小板中起与稳态作用相关的组成性作用,而后者主要负责诱导炎症作用。由于 COX-2 在炎性疾病的发病机制中起重要作用,因此它已被认为是抗炎中间体规划的目标。许多开发和计划用于 COX-2 抑制的抑制剂已经对人类产生副作用,主要是在胃肠道和/或心血管道。因此,有必要设计新的潜在COX-2抑制剂,相对安全且无副作用。从这个意义上说,塞来昔布是唯一一种有效的、选择性的 COX-2 抑制剂,仍然可以在市场上买到(在“coxib”家族中)。因此,塞来昔布成为开发 COX-2 酶抗炎剂的商业原型抑制剂。这篇综述提供了抑制亮点,为设计有前景的新型非甾体抗炎药 (NSAIDs) 提供了结构基础,这些药物作为 COX-2 抑制剂,对人体的副作用较小。
更新日期:2021-09-10
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