title: Small-molecule inhibitors/modulators of amyloid-β peptide aggregation and toxicity for the treatment of Alzheimer's disease: a patent review (2010 - 2012).
abstract: BACKGROUND
  Genetic, physiological, and biochemical data indicate that agglomerates of the 42-amino acid form of the amyloid-β (Aβ(42)) peptide are strongly linked to Alzheimer's disease (AD) etiology and thus represent a particularly attractive target for the development of an effective disease-modifying approach for AD treatment. A plethora of chemical entities able to modulate Aβ(42) self-assembly have been developed in recent years, among them, several are in clinical or preclinical development.
  
  
  METHODS
  This review accounts for small-molecule inhibitors of Aβ peptide polymerization and toxicity, reported in the patent literature during the 2010 - 2012 period, and their potential use as disease-modifying therapeutics for AD cure.
  
  
  CONCLUSIONS
  The earliest pathogenic event is the formation of soluble Aβ oligomers that disrupt synaptic communication. Drug design strategies targeting these primary toxic agents could hold considerable promises for obtaining effective anti-AD drugs candidate. The heterogeneous aggregation of Aβ and the resulting difficulty to structurally characterize the peptide represent important drawbacks.
authors: Alma MaterStudiorum-Bologna University, Department of Pharmacy and Biotechnologies, Bologna, Italy. federica.belluti@unibo.it
authors: Federica
authors: F
authors: Belluti
authors: Angela
authors: A
authors: Rampa
authors: Silvia
authors: S
authors: Gobbi
authors: Alessandra
authors: A
authors: Bisi
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy* / Q000503:physiopathology; D016229:Amyloid beta-Peptides / Q000187:drug effects* / Q000378:metabolism; D000818:Animals; D015195:Drug Design; D006801:Humans; D058990:Molecular Targeted Therapy; D010330:Patents as Topic; D010446:Peptide Fragments / Q000187:drug effects* / Q000378:metabolism; D013569:Synapses / Q000378:metabolism
chemical_list: D016229:Amyloid beta-Peptides; D010446:Peptide Fragments; C075222:amyloid beta-protein (1-42)