Thiacalix[4]arene as molecular platform for design of alkaline phosphatase inhibitors

Effect of thiacalix[4]arene platform on inhibition of alkaline phosphatase by macrocyclic phosphonate is presented in this article. Using tetrakis(dihydroxyphosphorylmethyl) derivatives we have found that phosphonate inhibitor on thiacalix[4]arene platform has displayed stronger inhibition propertie...

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Bibliographic Details
Published in:Journal of Inclusion Phenomena and Macrocyclic Chemistry 2010-04, Vol.66 (3-4), p.271-277
Main Authors: Vovk, A. I., Kononets, L. A., Tanchuk, V. Yu, Drapailo, A. B., Kalchenko, V. I., Kukhar, V. P.
Format: Article
Language:English
Subjects:
Chemistry
Chemistry and Materials Science
Crystallography and Scattering Methods
Food Science
Organic Chemistry
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Summary:Effect of thiacalix[4]arene platform on inhibition of alkaline phosphatase by macrocyclic phosphonate is presented in this article. Using tetrakis(dihydroxyphosphorylmethyl) derivatives we have found that phosphonate inhibitor on thiacalix[4]arene platform has displayed stronger inhibition properties towards alkaline phosphatases from bovine intestine mucosa, shrimp and human placenta than its structural calix[4]arene analogue. For elucidation of the molecular mechanism of the inhibition the tested macrocyclic compounds were docked computationally to the active site of alkaline phosphatase from shrimp. The role of thiacalix[4]arene platform in formation of the enzyme-inhibitor complex is discussed. Graphical Abstract Thiacalix[4]arene as molecular platform for design of alkaline phosphatase inhibitors
ISSN:0923-0750
1573-1111
DOI:10.1007/s10847-009-9607-9