TY  -  
T1  - Discovery of Membrane-Bound Pyrophosphatase Inhibitors Derived from an Isoxazole Fragment 
SN  -  /  
UR  - http://hdl.handle.net/10138/314686 
T3  -  
A1  - Johansson, Niklas G; Turku, Ainoleena; Vidilaseris, Keni; Dreano, Loic; Khattab, Ayman; Ayuso Perez, Daniel; Wilkinson, Aaron; Zhang, Yuezhou; Tamminen, Matti; Grazhdankin, Evgeni; Kiriazis, Alexandros; Fishwick, Colin W. G.; Meri, Seppo; Yli-Kauhaluoma, Jari; Goldman, Adrian; Boije af Gennäs, Gustav; Xhaard, Henri 
A2  -  
PB  -  
Y1  - 2020 
LA  - eng 
AB  - Membrane-bound pyrophosphatases (mPPases) regulate energy homeostasis in pathogenic protozoan parasites and lack human homologues, which makes them promising targets in e.g. malaria. Yet only few nonphosphorus inhibitors have been reported so far. Here, we explore an isoxazole fragment hit, leading to the discovery of small mPPase inhibitors with 6-10 mu M IC50 values in the Thermotoga maritima test system. Promisingly, the compounds retained activity against Plasmodium falciparum mPPase in memb... 
VO  -  
IS  -  
SP  -  
OP  -  
KW  - ACIDOCALCISOMES; BISPHOSPHONATES; Membrane-bound pyrophosphatase; PUMPING PYROPHOSPHATASES; TARGET; TRYPANOSOMA-BRUCEI; drug design; isoxazoles; protozoan diseases; 317 Pharmacy 
N1  -   
PP  -  
ER  -