title: Galectin-1 inhibitors and their potential therapeutic applications: a patent review.
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: a Institute for Glycomics , Griffith University , Gold Coast Campus , Queensland , Australia.
authors.forename: Helen
authors.initials: H
authors.lastname: Blanchard
authors.affiliation: a Institute for Glycomics , Griffith University , Gold Coast Campus , Queensland , Australia.
authors.forename: Khuchtumur
authors.initials: K
authors.lastname: Bum-Erdene
authors.affiliation: a Institute for Glycomics , Griffith University , Gold Coast Campus , Queensland , Australia.
authors.forename: Mohammad Hussaini
authors.initials: MH
authors.lastname: Bohari
authors.affiliation: a Institute for Glycomics , Griffith University , Gold Coast Campus , Queensland , Australia.
authors.forename: Xing
authors.initials: X
authors.lastname: Yu
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000494:pharmacology; D016503:Drug Delivery Systems; D015195:Drug Design; D037483:Galectin 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D007249:Inflammation / Q000188:drug therapy* / Q000473:pathology; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D010330:Patents as Topic; D011506:Proteins / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D037483:Galectin 1; D011506:Proteins
keywords: Galectin-1; carbohydrate; inhibitor design; patents