Galectin-1 inhibitors and their potential therapeutic applications: A patent review

No Thumbnail Available
File version
Author(s)
Blanchard, Helen
Bum-Erdene, Khuchtumur
Bohari, Mohammad Hussaini
Yu, Xing
Primary Supervisor
Other Supervisors
Editor(s)
Date
2016
Size
File type(s)
Location
License
Abstract

Introduction: Galectins have affinity for β-galactosides. Human galectin-1 is ubiquitously expressed in the body and its expression level can be a marker in disease. Targeted inhibition of galectin-1 gives potential for treatment of inflammatory disorders and anti-cancer therapeutics. Areas covered: This review discusses progress in galectin-1 inhibitor discovery and development. Patent applications pertaining to galectin-1 inhibitors are categorised as monovalent- and multivalent-carbohydrate-based inhibitors, peptides- and peptidomimetics. Furthermore, the potential of galectin-1 protein as a therapeutic is discussed along with consideration of the unique challenges that galectin-1 presents, including its monomer-dimer equilibrium and oxidized and reduced forms, with regard to delivering an intact protein to a pathologically relevant site. Expert opinion: Significant evidence implicates galectin-1’s involvement in cancer progression, inflammation, and host-pathogen interactions. Conserved sequence similarity of the carbohydrate-binding sites of different galectins makes design of specific antagonists (blocking agents/inhibitors of function) difficult. Key challenges pertaining to the therapeutic use of galectin-1 are its monomer-dimer equilibrium, its redox state, and delivery of intact galectin-1 to the desired site. Developing modified forms of galectin-1 has resulted in increased stability and functional potency. Gene and protein therapy approaches that deliver the protein toward the target are under exploration as is exploitation of different inhibitor scaffolds.

Journal Title

Expert Opinion on Therapeutic Patents

Conference Title
Book Title
Edition
Volume

26

Issue

5

Thesis Type
Degree Program
School
Publisher link
Patent number
Funder(s)
Grant identifier(s)
Rights Statement
Rights Statement
Item Access Status
Note
Access the data
Related item(s)
Subject

Biomedical engineering

Pharmacology and pharmaceutical sciences

Pharmacology and pharmaceutical sciences not elsewhere classified

Persistent link to this record
Citation
Collections