Potent Memapsin 2 (β-Secretase) Inhibitors: Design, Synthesis, Protein-Ligand X-ray Structure and in vivo Evaluation

Structure-based design, synthesis and biological evaluation of a series of peptidomimetic β–secretase inhibitors incorporating hydroxyethylamine isosteres are described. We have identified inhibitor 24 which has shown exceedingly potent activity in memapsin 2 enzyme inhibitory (K(i) 1.8 nM) and cell...

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Detalhes bibliográficos
Main Authors: Ghosh, Arun K., Kumaragurubaran, Nagaswamy, Hong, Lin, Kulkarni, Sarang, Xu, Xiaoming, Miller, Heather B., Reddy, Dandepally Srinivasa, Weerasena, Vajira, Turner, Robert, Chang, Wanpin, Koelsch, Gerald, Tang, Jordan
Formato: Artigo
Idioma:Inglês
Publicado em: 2008
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC2577816/
https://ncbi.nlm.nih.gov/pubmed/18180160
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2007.12.028
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