Discovery and optimization of the first highly effective and orally available galectin-3 inhibitors for treatment of fibrotic disease
FR Zetterberg, A MacKinnon, T Brimert… - Journal of Medicinal …, 2022 - ACS Publications
Galectin-3 is a carbohydrate-binding protein central to regulating mechanisms of diseases
such as fibrosis, cancer, metabolic, inflammatory, and heart disease. We recently found a …
such as fibrosis, cancer, metabolic, inflammatory, and heart disease. We recently found a …
A selective galactose–coumarin-derived galectin-3 inhibitor demonstrates involvement of galectin-3-glycan interactions in a pulmonary fibrosis model
VK Rajput, A MacKinnon, S Mandal… - Journal of medicinal …, 2016 - ACS Publications
Synthesis of doubly 3-O-coumarylmethyl-substituted thiodigalactosides from bis-3-O-
propargyl-thiodigalactoside resulted in highly selective and high affinity galectin-3 inhibitors …
propargyl-thiodigalactoside resulted in highly selective and high affinity galectin-3 inhibitors …
Dissecting the structure–activity relationship of galectin–ligand interactions
YC Chan, HY Lin, Z Tu, YH Kuo, STD Hsu… - International journal of …, 2018 - mdpi.com
Galectins are β-galactoside-binding proteins. As carbohydrate-binding proteins, they
participate in intracellular trafficking, cell adhesion, and cell–cell signaling. Accumulating …
participate in intracellular trafficking, cell adhesion, and cell–cell signaling. Accumulating …
Galectin‐3‐binding glycomimetics that strongly reduce bleomycin‐induced lung fibrosis and modulate intracellular glycan recognition
Discovery of glycan‐competitive galectin‐3‐binding compounds that attenuate lung fibrosis
in a murine model and that block intracellular galectin‐3 accumulation at damaged vesicles …
in a murine model and that block intracellular galectin‐3 accumulation at damaged vesicles …
[HTML][HTML] The therapeutic potential of galectin-3 inhibition in fibrotic disease
RJ Slack, R Mills, AC Mackinnon - … Journal of Biochemistry & Cell Biology, 2021 - Elsevier
Galectin-3 is a beta-galactoside-binding mammalian lectin and part of the 15 member
galectin family that are evolutionarily highly conserved. It is the only chimeric protein with a …
galectin family that are evolutionarily highly conserved. It is the only chimeric protein with a …
An updated patent review of galectin-1 and galectin-3 inhibitors and their potential therapeutic applications (2016–present)
A Sethi, S Sanam, R Alvala, M Alvala - Expert Opinion on …, 2021 - Taylor & Francis
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 …
protein family of high therapeutic potential and play a role in a wide variety of diseases like …
Synthesis, structure–activity relationships, and in vivo evaluation of novel tetrahydropyran-based thiodisaccharide mimics as galectin-3 inhibitors
L Xu, RA Hartz, BR Beno, K Ghosh… - Journal of Medicinal …, 2021 - ACS Publications
Galectin-3 is a member of a family of β-galactoside-binding proteins. A substantial body of
literature reports that galectin-3 plays important roles in cancer, inflammation, and fibrosis …
literature reports that galectin-3 plays important roles in cancer, inflammation, and fibrosis …
Targeting galectin-driven regulatory circuits in cancer and fibrosis
KV Mariño, AJ Cagnoni, DO Croci… - Nature Reviews Drug …, 2023 - nature.com
Galectins are a family of endogenous glycan-binding proteins that have crucial roles in a
broad range of physiological and pathological processes. As a group, these proteins use …
broad range of physiological and pathological processes. As a group, these proteins use …
Galectin-1 inhibitors and their potential therapeutic applications: a patent review
H Blanchard, K Bum-Erdene, MH Bohari… - Expert Opinion on …, 2016 - Taylor & Francis
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 …
expressed in the body and its expression level can be a marker in disease. Targeted …
Safety and pharmacokinetics of GB1211, an oral galectin-3 inhibitor: a single-and multiple-dose first-in-human study in healthy participants
V Aslanis, RJ Slack, AC MacKinnon… - Cancer Chemotherapy …, 2023 - Springer
Abstract Purpose Galectin-3, a β-galactoside-binding lectin, plays a key role in several
cellular pathways involved in chronic inflammation, heart disease and cancer. GB1211 is an …
cellular pathways involved in chronic inflammation, heart disease and cancer. GB1211 is an …