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引用次数: 0
摘要
导言:半胱氨酸蛋白酶参与了从细胞外基质周转到免疫等广泛的生物功能。半胱氨酸蛋白酶在癌症、免疫相关疾病、神经退行性疾病、病毒和寄生虫感染等多种疾病的发生和发展过程中发挥着重要作用,是开发治疗工具的一个极具吸引力的药物靶点:综述了近期关于设计和研究具有潜在治疗用途的半胱氨酸蛋白酶抑制剂的科学和专利文献:发现了许多有效的结构多样的半胱氨酸蛋白酶抑制剂,为开发治疗工具带来了新的挑战和机遇。一些蛋白酶单独或与抑制剂复合物的机理研究和 X 射线晶体结构为合理设计和开发高效、选择性半胱氨酸蛋白酶抑制剂提供了重要信息,这些抑制剂可作为治疗不同疾病的临床前候选药物。
Therapeutic cysteine protease inhibitors: a patent review (2018-present).
Introduction: Cysteine proteases are involved in a broad range of biological functions, ranging from extracellular matrix turnover to immunity. Playing an important role in the onset and progression of several diseases, including cancer, immune-related and neurodegenerative disease, viral and parasitic infections, cysteine proteases represent an attractive drug target for the development of therapeutic tools.
Areas covered: Recent scientific and patent literature focusing on the design and study of cysteine protease inhibitors with potential therapeutic application has been reviewed.
Expert opinion: The discovery of a number of effective structurally diverse cysteine protease inhibitors opened up new challenges and opportunities for the development of therapeutic tools. Mechanistic studies and the availability of X-ray crystal structures of some proteases, alone and in complex with inhibitors, provide crucial information for the rational design and development of efficient and selective cysteine protease inhibitors as preclinical candidates for the treatment of different diseases.
期刊介绍:
Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature.
The Editors welcome:
Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area
Patent Evaluations examining the aims and chemical and biological claims of individual patents
Perspectives on issues relating to intellectual property
The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D
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