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

Autor:	Andrew D. Mesecar, Emilio L. Cárdenas, Deborah Downs, Kanury V. S. Rao, Yu-Chen Yen, Xiangping Huang, Jordan Tang, Arun K. Ghosh, Bhavanam Sekhara Reddy
Rok vydání:	2016
Předmět:	0301 basic medicine Cathepsin Chemistry General Chemistry Type 2 diabetes Pharmacology Highly selective medicine.disease Combinatorial chemistry 3. Good health 03 medical and health sciences Memapsin 1 030104 developmental biology β secretase medicine
Zdroj:	Chemical Science. 7:3117-3122
ISSN:	2041-6539 2041-6520
DOI:	10.1039/c5sc03718b
Popis:	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 >170000-fold selectivity over β-secretase (BACE 1) and >15000-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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::573b8d66f02273c2c3c567ed0e16a2b0 https://doi.org/10.1039/c5sc03718b Zobrazit plný text záznamu