Design, Synthesis and Activity Study of Aminopeptidase N Targeted AHPA Derivatives
News Apr 26, 2012
A series of (2RS,3S)-3-amino- 2-hydroxy-4-phenyl-butanoic acids (AHPA) derivatives (MA0-MA7) were synthesized. The in vitro aminopeptidase N (APN) enzyme and cell proliferation assay of target compounds were investigated. The results showed that most compounds displayed potent inhibitory activities against APN, compound MA0 showed even better inhibitory effects than bestatin on both enzyme activity and HL60 cell proliferation. The FlexX docking result showed the mode of binding between MA0 and APN.
This study was published online in Drug Discoveries and Therapeutics and is free to access.
Stereochemistry is a science of reflection. Two chemical molecules with the same composition and structure, but with one as the mirror image of the other, can produce wildly varying effects. But University of Utah chemist Matt Sigman has been developing a way to get a better grasp on this tricky field of chemistry.READ MORE