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Updated: Jun 13, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
Published on: June 30, 2013
Tetrapeptides, as small-sized peptidic inhibitors; synthesis and their inhibitory activity against BACE1
Taeko Kakizawa1, Koushi Hidaka, Daisuke Hamada
1Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto, Japan.
Abstract:
Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) is known to be involved in the production of amyloid beta-peptide in Alzheimer's disease and is a major target for current drug design. We previously reported substrate-based peptidomimetics, KMI-compounds as potent BACE1 inhibitors. In this study, we designed and synthesized tetrapeptides as low molecular-sized inhibitors. These exhibited high potency against recombinant BACE1, with the highest IC(50) value of 34.6 nM from KMI-927.
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