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

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.

KEYWORDS:

• Galectins
• galectin-1
• galectin-3
• inhibitors
• patents

Article Highlights

• Galectins are a family of lectins found to regulate host defence mechanism positively and negatively against pathogens in addition to regulating cell adhesion, migration, proliferation, survival and cell death.

• There is considerable literature which depicts that galectins play an instrumental role in chronic inflammation, apoptosis, immune response, tumour, atherosclerosis, microbial infection, leukemia, multiple myeloma, lung fibrosis, and viral infections.

• This review focuses on the patents of the last 5 years pertaining to inhibitors of galectin-1 and galectin-3, two of the most widely studied isoforms within the galectin family.

• The structural perspectives in the design of specific galectin inhibitors have also been discussed.

This box summarizes key points contained in the article.

Acknowledgments

A.S. & S.S. would like to thank DoP, Government of India for grant of fellowship.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

A reviewer on this manuscript has disclosed that they have filed a related provisional patent. All other peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

No external funding received.