Development and Structural Modification of BACE1 Inhibitors

Molecules. 2016 Dec 22;22(1):4. doi: 10.3390/molecules22010004.

Abstract

Alzheimer's disease (AD) is a progressive neurodegenerative disorder which usually occurs in the elderly. The accumulation of β-amyloid and the formation of neurofibrillary tangles are considered as the main pathogenies of AD. Research suggests that β-secretase 1 (BACE1) plays an important role in the formation of β-amyloid. Discovery of new BACE1 inhibitors has become a significant method to slow down the progression of AD or even cure this kind of disease. This review summarizes the different types and the structural modification of these new BACE1 inhibitors.

Keywords: Alzheimer’s disease; BACE1; BACE1 inhibitors; structural modification; β-amyloid.

Publication types

  • Review

MeSH terms

  • Alkaloids / chemical synthesis
  • Alkaloids / pharmacology
  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / metabolism
  • Alzheimer Disease / pathology
  • Amyloid Precursor Protein Secretases / antagonists & inhibitors*
  • Amyloid Precursor Protein Secretases / biosynthesis
  • Amyloid Precursor Protein Secretases / genetics
  • Amyloid beta-Peptides / antagonists & inhibitors
  • Amyloid beta-Peptides / biosynthesis
  • Amyloid beta-Peptides / genetics
  • Aspartic Acid / chemistry
  • Aspartic Acid / metabolism
  • Aspartic Acid Endopeptidases / antagonists & inhibitors*
  • Aspartic Acid Endopeptidases / biosynthesis
  • Aspartic Acid Endopeptidases / genetics
  • Curcumin / chemical synthesis
  • Curcumin / pharmacology
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Gene Expression
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Neuroprotective Agents / chemical synthesis*
  • Neuroprotective Agents / pharmacology
  • Peptidomimetics / chemical synthesis*
  • Peptidomimetics / pharmacology
  • Piperazines / chemical synthesis
  • Piperazines / pharmacology
  • Structure-Activity Relationship
  • Terpenes / chemical synthesis
  • Terpenes / pharmacology

Substances

  • Alkaloids
  • Amyloid beta-Peptides
  • Enzyme Inhibitors
  • Neuroprotective Agents
  • Peptidomimetics
  • Piperazines
  • Terpenes
  • Aspartic Acid
  • Amyloid Precursor Protein Secretases
  • Aspartic Acid Endopeptidases
  • BACE1 protein, human
  • Curcumin