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Peroxo Compounds of Vanadium(V) and Niobium(V) as Potent Inhibitors of Calcineurin Activity towards RII-Phosphopeptide

Saikia, Gangutri and Gogoi, Sandhya Rani and Baruah, Jeena Jyoti and Ram, Babul Moni and Begum, Pakiza and Ahmed, Kabirun and Sharma, Mitu and Ramakrishna, Gayatri and Ramasarma, Tangirala and Islam, Nashreen S (2017) Peroxo Compounds of Vanadium(V) and Niobium(V) as Potent Inhibitors of Calcineurin Activity towards RII-Phosphopeptide. In: CHEMISTRYSELECT, 2 (21). pp. 5838-5848.

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Official URL: http://doi.org/10.1002/slct.201700935


Calcineurin (CN) is a major calmodulin binding serine/threonine phosphatase which plays a crucial role in numerous mammalian signal transduction pathways. Calcineurin inhibitors represent a valuable tool for elucidating CN dependent cellular processes. The present work deals with the synthesis and comprehensive characterization of a new polymer anchored peroxo niobium complex, Nb-2(O-2)(6)(carboxylate)(2)]-PA (Nb-2) PA=poly(sodium acrylate)], and identification of a set comprising of neat homoleptic as well as polymer immobilized peroxo complexes of vanadium(V) and niobium(V) as potent CN inhibitors. The in-vitro effect of the complexes on calmodulin mediated dephosphorylation activity of CN was investigated using a physiological substrate of calcineurin, RII-phosphopeptide as well as a non-protein substrate p-nitrophenyl phosphate (p-NPP). Enzyme kinetic analysis data revealed that the compounds inhibit function of CN via uncompetitive pathway with K-i values ranging between 1-3M, suggesting the formation of an enzyme-inhibitor-substrate complex during the course of inhibition.

Item Type: Journal Article
Additional Information: Copy right for this article belongs to the WILEY-V C H VERLAG GMBH, POSTFACH 101161, 69451 WEINHEIM, GERMANY
Department/Centre: Division of Biological Sciences > Biochemistry
Date Deposited: 24 Aug 2017 06:15
Last Modified: 16 Oct 2018 08:49
URI: http://eprints.iisc.ac.in/id/eprint/57668

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