[Calix[4]arene methylenebisphosphonic acids: the features of alkaline phosphatases inhibition].
The inhibition of alkaline phosphatases by calix[4]arenes functionalysed at the macrocyclic upper rim by one or two methylenebisphosphonic acid fragments has been investigated. It is established, that calix[4]arene bismethylenebisphosphonic acid displayed stronger inhibition of alkaline phosphatase from bovine intestine mucosa than calix[4]arene methylenebisphosphonic acid. At the same time, the both inhibitors showed almost similar levels of inhibitory activities in respect of bovine kidney alkaline phosphatase or E. coli alkaline phosphatase. The tested compounds were docked computationally to the active site of the E. coli alkaline phosphatase. On the basis of results obtained the possible binding modes of inhibitors were analysed.
Muzychka
O V
OV
Tanchuk
V Iu
VIu
Vovk
A I
AI
Muravĭova
I V
IV
Cherenok
S O
SO
Kal'chenko
V I
VI
Kukhar
V P
VP
D000469:Alkaline Phosphatase / Q000037:antagonists & inhibitors*; D000818:Animals; D001665:Binding Sites; D047250:Calixarenes / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000201:enzymology; D007413:Intestinal Mucosa / Q000201:enzymology; D007421:Intestine, Small / Q000201:enzymology; D007668:Kidney / Q000201:enzymology; D008958:Models, Molecular; D015394:Molecular Structure; D009943:Organophosphorus Compounds / Q000494:pharmacology*; D010636:Phenols / Q000737:chemistry / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D009943:Organophosphorus Compounds; D010636:Phenols; C121325:calix(4)arene; D047250:Calixarenes; D000469:Alkaline Phosphatase