O. V. Muzychka1, V. Yu. Tanchuk1, A. I. Vovk1, I. V. Muravyova1, S. A. Cherenok2, V. I. Kalchenko2, V. P. Kukhar1
The inhibition of alkaline phosphatases by calixarenes functionalysed at the macrocyclic upper rim by one or two methylenebisphosphonic acid fragments has been investigated. It is established, that calixarene bismethylenebisphosphonic acid displayed stronger inhibition of alkaline phosphatase from bovine intestine mucosa than calixarene 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.
Кey words: alkaline phosphatase, inhibitors, methylenebisphosphonic acids, calixarenes, molecular docking.
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