Work

Design of potent and highly selective inhibitors for human β-secretase 2 (memapsin 1), a target for type 2 diabetes

Year: 2016

Type: article

Abstract: Design, synthesis and evaluation of very potent and selective β-Secretase 2 (memapsin 1, BACE 2) inhibitors are described. The inhibitors were designed specifically to interact with the S2'-site of β-secretase 2 to provide >170,000-fold selectivity over β-secretase (BACE 1) and >15,000-fold selectivity over cathepsin D. BACE 2 is implicated in Type 2 diabetes. The studies serve as an important guide to selective BACE 2 inhibitors.

Source: Chemical Science

DOI: 10.1039/c5sc03718b

Authors: Arun K. Ghosh, Bhavanam Sekhara Reddy, Yu-Chen Yen, Emilio L. Cárdenas, Kalapala Venkateswara Rao, Deborah Downs, Xiangping Huang, Jordan Tang, Andrew D. Mesecar

Institutions: Purdue University West Lafayette, Oklahoma Medical Research Foundation, University of Oklahoma

Language: English

Topic: Alzheimer's disease research and treatments

Subfield: Physiology

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: diamond

Funders: U.S. Department of Energy, Walther Cancer Foundation, Michigan Economic Development Corporation, Purdue University, National Institutes of Health, Office of Science, National Institute on Aging, National Cancer Institute, National Institute of General Medical Sciences, National Institute of Allergy and Infectious Diseases, Argonne National Laboratory

Awards: G102163711, Novel Protease Inhibitors as SARS Therapeutics, G1313983767, G2499798185, G2896567508, G498139845, Cancer Center Support Grant, Design & Synthesis of Nonpeptide Protease Inhibitors, Beta Secretase Inhibition for Treating Alzheimer's Disease, G9000172862, G969889393

OpenAlex ID: W2264627017

FWCI: 2.146

Cites: 35

Cited by: 15

Related to: 10