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Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Sci+Rep 2016 ; 6 (ä): ä Nephropedia Template TP
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Structure of neprilysin in complex with the active metabolite of sacubitril #MMPMID27302413
Sacubitril is an ethyl ester prodrug of LBQ657, the active neprilysin (NEP) inhibitor, and a component of LCZ696 (sacubitril/valsartan). We report herein the three-dimensional structure of LBQ657 in complex with human NEP at 2?Å resolution. The crystal structure unravels the binding mode of the compound occupying the S1, S1? and S2? sub-pockets of the active site, consistent with a competitive inhibition mode. An induced fit conformational change upon binding of the P1?-biphenyl moiety of the inhibitor suggests an explanation for its selectivity against structurally homologous zinc metallopeptidases.