title: Galectin-3 inhibitors: a patent review (2008-present).
abstract: BACKGROUND
  Galectin-3 (Gal-3), a lectin with preference for β-galactoside-containing carbohydrates, is a structurally unique member of the galectin family. It is ubiquitously expressed in various mammalian tissues with a wide distribution from the intracellular environment to the extracellular space. Gal-3 is a well-established player in numerous diseases, from infections to heart failure. Notably, as Gal-3 overexpression is associated with cancer drug resistance, it has been identified as a valuable therapeutic target in the fight against cancers.
  
  
  METHODS
  This review discusses the recent progress of patent applications (2008-present) and the current knowledge of pertinent Gal-3-inhibitor interactions in an effort to progress the development of selective and high affinity carbohydrate-based inhibitors targeting Gal-3, with an emphasis on engaging a structure-based drug design rationale.
  
  
  CONCLUSIONS
  The lack of commercially available anti-Gal-3 therapeutic reagents and its clear involvement in serious disease, notably cancer, leads to an urgent need for development of inhibitors that specifically target Gal-3. Design of potent and selective carbohydrate inhibitors targeting Gal-3 is challenging due to relative weak protein-carbohydrate interactions along with the high sequence homology in the carbohydrate binding site region among galectins. To date, some chemical scaffolds have been exploited for design of promising effective Gal-3 inhibitors for cancer therapy.
authors.affiliation: Griffith University, Institute for Glycomics , Gold Coast Campus, Queensland 4222 , Australia +617 555 27023 ; +617 555 28098 ; h.blanchard@griffith.edu.au.
authors.forename: Helen
authors.initials: H
authors.lastname: Blanchard
authors.forename: Xing
authors.initials: X
authors.lastname: Yu
authors.forename: Patrick Michael
authors.initials: PM
authors.lastname: Collins
authors.forename: Khuchtumur
authors.initials: K
authors.lastname: Bum-Erdene
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D002986:Clinical Trials as Topic; D018360:Crystallography, X-Ray; D015195:Drug Design; D037502:Galectin 3 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D010330:Patents as Topic; D017434:Protein Structure, Tertiary
chemical_list: D000970:Antineoplastic Agents; D037502:Galectin 3
keywords: carbohydrate; galectin; inhibitor design; patents