Imperial College London
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Dr Woscholski

Faculty of Natural Sciences, Department of Chemistry

Reader in Chemical Biology
 
 
 
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Contact

 

+44 (0)20 7594 5305r.woscholski

 
 
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Location

 

301LMolecular Sciences Research HubWhite City Campus

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Summary

 

Publications

Citation

BibTex format

@article{Vilar:2016:10.1039/C5DT04753F,
author = {Vilar, Compte R and Collins, J and Woscholski, R and Cilibrizzi, A and Leatherbarrow, RJ and Fedorova, M and Whyte, G and Guterman, I and Mak, LH},
doi = {10.1039/C5DT04753F},
journal = {Dalton Transactions},
pages = {7104--7113},
title = {Vanadyl complexes with dansyl-labelled di-picolinic acid ligands: synthesis, phosphatase inhibition activity and cellular uptake studies},
url = {http://dx.doi.org/10.1039/C5DT04753F},
volume = {45},
year = {2016}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - 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  dipicolinic  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.
AU  - Vilar,Compte R
AU  - Collins,J
AU  - Woscholski,R
AU  - Cilibrizzi,A
AU  - Leatherbarrow,RJ
AU  - Fedorova,M
AU  - Whyte,G
AU  - Guterman,I
AU  - Mak,LH
DO  - 10.1039/C5DT04753F
EP  - 7113
PY  - 2016///
SN  - 1477-9226
SP  - 7104
TI  - Vanadyl complexes with dansyl-labelled di-picolinic acid ligands: synthesis, phosphatase inhibition activity and cellular uptake studies
T2  - Dalton Transactions
UR  - http://dx.doi.org/10.1039/C5DT04753F
UR  - http://hdl.handle.net/10044/1/30274
VL  - 45
ER  -
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