Kopalli Spandana R, Kang Tae-Bong, Lee Kwang-Ho, Koppula Sushruta
College of Biomedical and Health Sciences, Konkuk University, Chungju. Korea.
Recent Pat Anticancer Drug Discov. 2018;13(1):106-117. doi: 10.2174/1574892812666171027102627.
Inflammasomes are recognized as key regulators in innate immunity from the pathogenic to endogenous danger signals. Although controlled activation of inflammasome is highly beneficial, dysregulation of inflammasome activation plays central role in various autoimmune, inflammatory disorders and aid in promoting various forms of cancers in humans such as breast cancer, fibrosarcoma, gastric carcinoma, and lung metastasis. NLRP3 inflammasome activation has been emerged as a topic of interest and is under profound investigation for its involvement in multiple forms of cancers.
This review emphasizes an overview of the recent patents on NLRP3 inflammasome activation inhibitors with their relevant biological/pharmacological properties for the prevention and treatment of inflammation-associated cancer disorders.
Data were obtained from online patent searchers such as World Intellectual Property Organization (WIPO®), Free Patent Online (FPO), Espacenet® and Google Patents.
Several NLRP3 inflammasome activation inhibitors were recently patented from naturally derived and synthetic agents mainly by academic researchers. Most of the claimed patents have been validated and confined to cell lines and animal models limiting their entry into clinical settings.
The vigorous effort to discover and develop agents to specifically inhibit NLRP3 inflammasome activation, may pave the way to therapeutic intervention targeting inflammasome-regulated pathways that are involved in the pathogenesis of various forms of cancer.
炎性小体被认为是先天性免疫中从病原体到内源性危险信号的关键调节因子。尽管炎性小体的受控激活非常有益，但炎性小体激活的失调在各种自身免疫性、炎性疾病中起核心作用，并有助于促进人类多种形式的癌症，如乳腺癌、纤维肉瘤、胃癌和肺转移。NLRP3炎性小体激活已成为一个受关注的话题，并且因其与多种形式癌症的关联而正在接受深入研究。
本综述着重概述了近期关于NLRP3炎性小体激活抑制剂的专利，及其预防和治疗炎症相关癌症疾病的相关生物学/药理学特性。
数据来自世界知识产权组织（WIPO®）、免费专利在线（FPO）、欧洲专利局专利数据库（Espacenet®）和谷歌专利等在线专利检索工具。
近期，主要由学术研究人员从天然来源和合成制剂中获得了几种NLRP3炎性小体激活抑制剂的专利。大多数所主张的专利已在细胞系和动物模型中得到验证，但限制了它们进入临床应用。
大力发现和开发特异性抑制NLRP3炎性小体激活的药物，可能为针对炎性小体调节途径的治疗干预铺平道路，这些途径参与了多种形式癌症的发病机制。
