title: Recent progress in the drug discovery of non-peptidic BACE1 inhibitors.
abstract: 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.
  
  
  METHODS
  In this review, we describe the design of non-peptidic BACE1 inhibitors from a historical perspective and not by the inhibitor's category.
  
  
  CONCLUSIONS
  The respective methods have both merits and demerits and should be used in a mutually complementary manner.
authors.affiliation: Kyoto Pharmaceutical University, Center for Frontier Research in Medicinal Science, Department of Medicinal Chemistry, Yamashina-ku, Kyoto, Japan.
authors.forename: Yoshio
authors.initials: Y
authors.lastname: Hamada
authors.forename: Yoshiaki
authors.initials: Y
authors.lastname: Kiso