Qiang Ren, Yiqing Fan, Lixin Yang, Mayu Shan, Wei Shi, Hai Qian
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引用次数: 0
Abstract
Introduction: Free fatty acid receptor 1 (FFAR1) is a potential therapeutic target for type 2 diabetes mellitus (T2DM) because it could clinically stimulate insulin release in a glucose-dependent manner without inducing hypoglycemia. In both the pharmaceutical industry and academic community, FFAR1 agonists have attracted considerable attention.
Areas covered: The review presents a patent overview of FFAR1 modulators in 2020-2023, along with chemical structures, the biological activities and therapeutic applications of the representative compounds. Our patent survey used the major electronic databases, namely SciFinder, and Web of Science and Innojoy.
Expert opinion: Although FFAR1 agonists exhibit outstanding advantages, they are also associated with significant challenges. At present, reducing the molecular weight and overall lipophilicity and developing tissue-specific FFAR1 agonists may be the strategies for alleviating hepatotoxicity.
引言：游离脂肪酸受体1（FFAR1）是2型糖尿病（T2DM）的潜在治疗靶点，因为它在临床上可以以葡萄糖依赖的方式刺激胰岛素释放，而不会诱发低血糖。在制药行业和学术界，FFAR1激动剂都引起了相当大的关注。涵盖领域：该综述介绍了2020-2023年FFAR1调节剂的专利概述，以及代表性化合物的化学结构、生物活性和治疗应用。我们的专利调查使用了主要的电子数据库，即SciFinder、Web of Science和Innojoy。专家意见：尽管FFAR1激动剂表现出突出的优势，但它们也面临着重大挑战。目前，降低分子量和整体亲脂性，开发组织特异性FFAR1激动剂可能是减轻肝毒性的策略。
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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