Recent progress in the drug discovery of non-peptidic BACE1 inhibitors
1Kyoto Pharmaceutical University, Center for Frontier Research in Medicinal Science, Department of Medicinal Chemistry, Yamashina-ku, Kyoto, Japan.
Background:
β-Secretase, also called BACE1, is a promising molecular target for developing anti-Alzheimer's disease drugs. Several approaches of drug discovery for this therapy have been attempted, for example, substrate-based and structure-based designs, high-throughput screening, fragment-based lead generation and in silico screening.
Method:
In this review, we describe the design of non-peptidic BACE1 inhibitors from a historical perspective and not by the inhibitor's category.
Conclusion:
The respective methods have both merits and demerits and should be used in a mutually complementary manner.
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