Background: Alzheimer’s disease (AD) is one of the neurodegenerative diseases and has
been hypothesized to be a protein misfolding disease. In the generation of AD, β-secretase, γ-secretase,
and tau protein play an important role. A literature search reflects ever increasing interest in the design
and development of anti-AD drugs targeting β-secretase, γ-secretase, and tau protein.
Objective: The objective is to explore the structural aspects and role of β-secretase, γ-secretase, and tau
protein in AD and the efforts made to exploit them for the design of effective anti-AD drugs.
Methods: The manuscript covers the recent studies on design and development of anti-AD drugs exploiting
amyloid and cholinergic hypotheses.
Results: Based on amyloid and cholinergic hypotheses, effective anti-AD drugs have been searched out
in which non-peptidic BACE1 inhibitors have been most prominent.
Conclusion: Further exploitation of the structural aspects and the inhibition mechanism for β-secretase,
γ-secretase, and tau protein and the use of cholinergic hypothesis may lead still more potent anti-AD