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Outline of gelatinase inhibitors as anti-cancer agents: A patent mini-review for 2010-present
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2020-11-24 , DOI: 10.1016/j.ejmech.2020.113044
Sandip Kumar Baidya , Sk. Abdul Amin , Tarun Jha

Matrix metalloproteinases (MMPs) are involved in several pathological and physiological functions. Gelatinase (MMP-2 and -9) have significant attention as a therapeutic target against cancer. Gelatinase inhibitors have demonstrated their effectiveness in several diseases including cancer. However, it is quite a challenging task to develop inhibitors as a therapeutic agent.

This review summarizes the patent dedicated to the medicinal chemistry of gelatinase inhibitor reported over last decades. We examine the patent being pursued for gelatinase inhibitor development to highlight the key issues. The main aim is to provide the scientific community with an overview of the patented gelatinase inhibitors to allow further development.

During early the 2000s, some MMP inhibitors failed to pass the clinical trials. Hence, the lessons learned from early evidence and recent knowledge in that field will project rejuvenate the development of the selective inhibitors. Various studies and patents have continued in the recent years to expand knowledge in that field. Continuously, our research team has been involved in the design of potent and selective gelatinase inhibitors for the past few years. This study is a part of our efforts. This study may be beneficial in the design and development of better gelatinase inhibitors in the future.



中文翻译:

明胶酶抑制剂作为抗癌药的概述:2010年至今的专利迷你审查

基质金属蛋白酶(MMPs)参与多种病理和生理功能。明胶酶(MMP-2和-9)作为治疗癌症的靶点已引起广泛关注。明胶酶抑制剂已证明其在包括癌症在内的多种疾病中的有效性。然而,开发抑制剂作为治疗剂是一项艰巨的任务。

这篇综述总结了过去几十年中报道的专门用于明胶酶抑制剂药物化学的专利。我们研究了明胶酶抑制剂开发中正在寻求的专利,以突出关键问题。其主要目的是为科学界提供获得专利的明胶酶抑制剂的概述,以便进一步开发。

在2000年代初期,一些MMP抑制剂未能通过临床试验。因此,从该领域的早期证据和最新知识中汲取的教训将使振兴选择性抑制剂的发展焕然一新。近年来,继续进行各种研究和专利以扩展该领域的知识。在过去的几年中,我们的研究团队不断地参与了有效和选择性明胶酶抑制剂的设计。这项研究是我们努力的一部分。这项研究可能对将来更好的明胶酶抑制剂的设计和开发有益。

更新日期:2020-11-25
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