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Vanadyl complexes with dansyl-labelled dipicolinic acid ligands: synthesis, phosphatase inhibition activity and cellular uptake studies

Collins, J, Cilibrizzi, A, Fedorova, M, Whyte, G, Mak, LH, Guterman, I, Leatherbarrow, RJ, Woscholski, R and Vilar, R (2016) Vanadyl complexes with dansyl-labelled dipicolinic acid ligands: synthesis, phosphatase inhibition activity and cellular uptake studies. Dalton Transactions, 45 (16). pp. 7104-7113. ISSN 1477-9226

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Abstract

Vanadium complexes have been previously utilised as potent inhibitors of cysteine based phosphatases (CBPs). Herein, we present the synthesis and characterisation of two new fluorescently labelled vanadyl complexes (14 and 15) with bridged di-picolinic acid ligand. These compounds differ significantly from previous vanadyl complexes with phosphatase inhibition properties in that the metal-chelating part is a single tetradentate unit, which should afford greater stability and scope for synthetic elaboration then the earlier complexes. These new complexes inhibit a selection of cysteine based phosphatases (CBPs) in the nM range with some selectivity. Fluorescence spectroscopic studies (including fluorescence anisotropy) were carried out to demonstrate that the complexes are not simply acting as vanadyl delivery vehicles but they interact with the proteins. Finally, we present preliminary fluorescence microscopy studies to demonstrate that the complexes are cell permeable and localise throughout the cytoplasm of NIH3T3 cells.

Item Type: Article
Uncontrolled Keywords: 0302 Inorganic Chemistry, 0399 Other Chemical Sciences
Subjects: Q Science > QD Chemistry
Q Science > QR Microbiology
Divisions: Vice-Chancellor's Office
Publisher: Royal Society of Chemistry
Related URLs:
Date Deposited: 20 Jun 2018 08:43
Last Modified: 20 Jun 2018 08:43
DOI or Identification number: 10.1039/c5dt04753f
URI: http://researchonline.ljmu.ac.uk/id/eprint/8860

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