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Galectin-1 和 galectin-3 抑制剂及其潜在治疗应用的最新专利审查(2016 年至今)。

An updated patent review of galectin-1 and galectin-3 inhibitors and their potential therapeutic applications (2016-present).

机构信息

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research-Hyderabad, Balanagar, India.

G Pulla Reddy College of Pharmacy, Mehdipatnam, Hyderabad, India.

出版信息

Expert Opin Ther Pat. 2021 Aug;31(8):709-721. doi: 10.1080/13543776.2021.1903430. Epub 2021 May 20.

DOI:10.1080/13543776.2021.1903430
PMID:33749494
Abstract

INTRODUCTION

Galectins are ubiquitous in nature. They have established themselves as a protein family of high therapeutic potential and play a role in a wide variety of diseases like cancer, fibrosis, and Alzheimer's. Within the galectin family, galectin- 1 and galectin- 3 have been widely studied and their roles and functions have now been well established.

AREAS COVERED

In this review, we discuss the important advancements in the development of galectin-1 & 3 inhibitors. All patents filed detailing the divergent strategies to inhibit galectin-1 & 3 from 2016 to present have been covered and discussed.

EXPERT OPINION

Over the past couple of decades, distinct galectin inhibitors have been synthesized, reported and studied. Among all, the mono and disaccharide-based antagonists have been found to be considerably successful. However, the cumbersome synthetic route followed to develop this class of inhibitors, in addition to complexity involved in making selective modifications within these molecules has posed a significant challenge. Recently, there have been numerous reports on heterocyclic-based galectin inhibitors. If these are established as potent galectin inhibitors, their ease of synthesis and tunability could overcome the potential drawbacks of carbohydrate-based inhibitors and could thus be exploited to develop efficient and highly specific galectin inhibitors.

摘要

简介

半乳糖凝集素在自然界中普遍存在。它们已成为具有高治疗潜力的蛋白质家族,在癌症、纤维化和阿尔茨海默病等多种疾病中发挥作用。在半乳糖凝集素家族中,半乳糖凝集素-1 和半乳糖凝集素-3 已得到广泛研究,其作用和功能现已得到充分证实。

涵盖领域

在这篇综述中,我们讨论了半乳糖凝集素-1 和 -3 抑制剂开发方面的重要进展。涵盖并讨论了 2016 年至今所有详细描述抑制半乳糖凝集素-1 和 -3 的不同策略的专利申请。

专家意见

在过去的几十年中,已经合成、报道和研究了不同的半乳糖凝集素抑制剂。在所有这些抑制剂中,单糖和二糖基拮抗剂被发现非常成功。然而,开发这类抑制剂所遵循的繁琐合成路线,以及在这些分子中进行选择性修饰所涉及的复杂性,都构成了重大挑战。最近,有许多关于杂环基半乳糖凝集素抑制剂的报道。如果这些抑制剂被证明是有效的半乳糖凝集素抑制剂,它们合成的简便性和可调节性可以克服基于碳水化合物抑制剂的潜在缺点,因此可以用来开发高效和高度特异性的半乳糖凝集素抑制剂。

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