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.
A New Tactic in the Fight Against Drug-Resistant InfectionsNews
$1 million research grant could lead to life-saving antibiotics.READ MORE
Concept Life Sciences Appoints New Group Head of ToxicologyNews
Appointment supports growth of the Company and expansion of expertise in integrated drug discovery and development.READ MORE