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Journal archive > 2007 > N 6 November-December

CALIX[4]ARENE METHYLENEBISPHOSPHONIC ACIDS: THE FEATURES
OF ALKALINE PHOSPHATASES INHIBITION

O. V. Muzychka1, V. Yu. Tanchuk1, A. I. Vovk1, I. V. Muravyova1, S.  A.  Cherenok2, V. I. Kalchenko2, V. P. Kukhar1

1Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Kyiv;
2Institute of Organic Chemistry, National Academy of Sciences of Ukraine, Kyiv;
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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.

Кey words: alkaline phosphatase, inhibitors, methylenebisphosphonic acids, calix[4]arenes, molecular docking.

The original article in Ukrainian is available for download in PDF format.

© The Ukrainian Biochemical Journal