Discovery of a series of selective and cell permeable beta-secretase (BACE1) inhibitors by fragment linking with the assistance of STD-NMR.
 

Discovery of a series of selective and cell permeable beta-secretase (BACE1) inhibitors by fragment linking with the assistance of STD-NMR.

http://www.bionmr.com//www.ncbi.nlm....PubMedLink.gif Related Articles Discovery of a series of selective and cell permeable beta-secretase (BACE1) inhibitors by fragment linking with the assistance of STD-NMR.

Bioorg Chem. 2019 11;92:103253

Authors: Fang WS, Sun DY, Yang S, Cheng C, Moschke K, Li T, Sun S, Lichtenthaler SF, Huang J, Wang Y

Abstract
Two ?-secreatase (BACE1) inhibitors from natural products (cinnamic acid and flavone) were linked to furnish potent, cell permeable BACE1 inhibitors with noncompetitive mode of inhibition, with the assistance of saturated transfer difference (STD)-NMR technique. Some of these conjugates also exhibited selective BACE1 inhibition over other aspartyl proteases such as BACE-2 and renin, as well as poor cytotoxicity. Taken together, conjugates 4 represent a new series of BACE inhibitors warrants further investigation for their potential in Alzheimier's disease therapy.


PMID: 31557620 [PubMed - indexed for MEDLINE]



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