Download MendeleyDesign of Potent and Highly Selective Inhibitors for Human beta-Secretase 2 (Memapsin 1), a Target for Type 2 Diabetes.
Ghosh, A.K., Reddy, B.S., Yen, Y.C., Cardenas, E., Rao, K.V., Downs, D., Huang, X., Tang, J., Mesecar, A.D.(2016) Chem Sci 7: 3117-3122
- PubMed: 27347366
- DOI: https://doi.org/10.1039/C5SC03718B
- Primary Citation of Related Structures:
5DQC - PubMed 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.
Organizational Affiliation:
Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907 (USA).
