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Journal articleRosivatz E, Matthews JG, McDonald NQ, et al., 2006,
A small molecule inhibitor for phosphatase and tensin homologue deleted on chromosome 10 (PTEN)
, ACS Chem.Biol., Vol: 1, Pages: 780-790Phosphatase and tensin homologue deleted on chromosome 10 (PTEN), a phosphoinositide 3-phosphatase, is an important regulator of insulin-dependent signaling. The loss or impairment of PTEN results in an antidiabetic impact, which led to the suggestion that PTEN could be an important target for drugs against type II diabetes. Here we report the design and validation of a small- molecule inhibitor of PTEN. Compared with other cysteine-based phosphatases, PTEN has a much wider active site cleft enabling it to bind the PtdIns(3,4,5)P3 substrate. We have exploited this feature in the design of vanadate scaffolds complexed to a range of different organic ligands, some of which show potent inhibitory activity. A vanadyl complexed to hydroxypicolinic acid was found to be a highly potent and specific inhibitor of PTEN that increases cellular PtdIns(3,4,5)P3 levels, phosphorylation of Akt, and glucose uptake in adipocytes at nanomolar concentrations. The findings presented here demonstrate the applicability of a novel and specific chemical inhibitor against PTEN in research and drug development
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Journal articleGimeno N, Vilar R, 2006,
Anions as templates in coordination and supramolecular chemistry
, COORDINATION CHEMISTRY REVIEWS, Vol: 250, Pages: 3161-3189, ISSN: 0010-8545- Author Web Link
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- Citations: 250
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Journal articleBurkill HA, Vilar R, White AJP, 2006,
Synthesis of a series of ruthenium and rhodium complexes with tridentate pyridine-based ligands containing hydrogen bonding groups
, INORGANICA CHIMICA ACTA, Vol: 359, Pages: 3709-3722, ISSN: 0020-1693- Author Web Link
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- Citations: 12
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Journal articleChristmann U, Pantazis DA, Benet-Buchholz J, et al., 2006,
Experimental and theoretical investigations of new dinuclear palladium complexes as precatalysts for the amination of aryl chlorides
, JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Vol: 128, Pages: 6376-6390, ISSN: 0002-7863- Author Web Link
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- Citations: 123
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Journal articleReed JE, Arnal AA, Neidle S, et al., 2006,
Stabilization of G-quadruplex DNA and inhibition of telomerase activity by square-planar nickel(II) complexes
, JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Vol: 128, Pages: 5992-5993, ISSN: 0002-7863- Author Web Link
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- Citations: 298
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Journal articleDíaz P, Benet-Buchholz J, Vilar R, et al., 2006,
Anion influence on the structures of a series of copper(II) metal-organic frameworks
, INORGANIC CHEMISTRY, Vol: 45, Pages: 1617-1626, ISSN: 0020-1669- Author Web Link
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- Citations: 127
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Journal articleMiller PW, Long NJ, de Mello AJ, et al., 2006,
Rapid formation of amides <i>via</i> carbonylative coupling reactions using a microfluidic device
, CHEMICAL COMMUNICATIONS, Pages: 546-548, ISSN: 1359-7345- Author Web Link
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- Citations: 84
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Conference paperMiller PW, Long NJ, De Mello AJ, et al., 2006,
Rapid gas-liquid palladium carbonylative cross-coupling reactions using a glass fabricated microfluidic chip for applications in 11C- radiolabelling
, Pages: 876-878A series of gas-liquid palladium catalysed carbonylative cross-coupling reactions, forming secondary amides, were carried out using a glass fabricated microfluidic device. Improved yields from the microreactions were obtained in short reaction times (< 2 min) and were higher in all cases when compared to their corresponding batch reactions. We are currently in the process of applying our reaction set-up to [<sup>11</sup>C]CO radiolabelling to be used in PET (Positron Emission Tomography) imaging. © 2006 Society for Chemistry and Micro-Nano Systems.
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Conference paperReed JE, Arola A, Vilar R, et al., 2005,
Metal-containing stabilisers of G-quadruplex DNA as telomerase inhibitors.
, 17th EORTC/AACR/NCI International Conference on Molecular Targets and Cancer Therapeutics, Publisher: AMER ASSOC CANCER RESEARCH, Pages: 9051S-9051S, ISSN: 1078-0432 -
Journal articleOwen GR, Burkill HA, Vilar R, et al., 2005,
Palladium complexes containing ligands with hydrogen-bonding functionalities. Reactivity and catalytic studies with CO and olefins
, Journal of Organometallic Chemistry, Vol: 690, Pages: 5113-5124, ISSN: 0022-328X -
Journal articleFormentín P, Gimeno N, Steinke JHG, et al., 2005,
Reactivity of Grubbs' catalysts with urea- and amide-substituted olefins.: Metathesis and isomerization
, JOURNAL OF ORGANIC CHEMISTRY, Vol: 70, Pages: 8235-8238, ISSN: 0022-3263- Author Web Link
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- Citations: 40
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Journal articleCoronado E, Galán-Mascaros JR, Martí-Gastaldo C, et al., 2005,
Reversible colorimetric probes for mercury sensing
, JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Vol: 127, Pages: 12351-12356, ISSN: 0002-7863- Author Web Link
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- Citations: 310
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Conference paperRosivatz E, Vilar R, Woscholski R, 2005,
Imaging of PKB phosphorylation as an <i>in vivo</i> readout for PTEN inhibition studies
, IUBMB 50th Anniversary Symposium, Publisher: BLACKWELL PUBLISHING, Pages: 313-313, ISSN: 1742-464X -
Journal articleBurkill HA, Robertson NR, Vilar R, et al., 2005,
Synthesis, structural characterization, and magnetic studies of polynuclear iron complexes with a new disubstituted pyridine ligand
, INORGANIC CHEMISTRY, Vol: 44, Pages: 3337-3346, ISSN: 0020-1669- Author Web Link
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- Citations: 24
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Journal articleTovilla JA, Vilar R, White AJP, 2005,
A di-palladium urea complex as a molecular receptor for anions
, CHEMICAL COMMUNICATIONS, Pages: 4839-4841, ISSN: 1359-7345- Author Web Link
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- Citations: 26
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Journal articleChristmann U, Vilar R, 2005,
Monoligated palladium species as catalysts in cross-coupling reactions
, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, Vol: 44, Pages: 366-374, ISSN: 1433-7851- Author Web Link
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- Citations: 718
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Journal articleDiaz P, Mingos DMP, Vilar R, et al., 2004,
Anion-templated synthesis of metallacages as a means for the colorimetric detection of chlorides
, INORGANIC CHEMISTRY, Vol: 43, Pages: 7597-7604, ISSN: 0020-1669- Author Web Link
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- Citations: 54
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Journal articleChristmann U, Vilar R, White AJP, et al., 2004,
Synthesis of two novel dinuclear palladium(I) complexes and studies of their catalytic activity in amination reactions
, CHEMICAL COMMUNICATIONS, Pages: 1294-1295, ISSN: 1359-7345- Author Web Link
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- Citations: 77
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Journal articleSchmid AC, Byrne RD, Vilar R, et al., 2004,
Bisperoxovanadium compounds are potent PTEN inhibitors
, FEBS LETTERS, Vol: 566, Pages: 35-38, ISSN: 1873-3468- Author Web Link
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- Citations: 188
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Journal articleRais D, Gould IR, Vilar R, et al., 2004,
Structural and theoretical studies of new ruthenium-amidato complexes with phenanthroline ligands containing H-bonding groups
, EUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Pages: 1865-1872, ISSN: 1434-1948- Author Web Link
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- Citations: 9
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Journal articlePalomares E, Vilar R, Durrant JR, 2004,
Heterogeneous colorimetric sensor for mercuric salts
, CHEMICAL COMMUNICATIONS, Pages: 362-363, ISSN: 1359-7345- Author Web Link
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- Citations: 162
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Journal articlePalomares E, Vilar R, Green A, et al., 2004,
Alizarin complexone on nanocrystalline TiO<sub>2</sub>:: A heterogeneous approach to anion sensing
, ADVANCED FUNCTIONAL MATERIALS, Vol: 14, Pages: 111-115, ISSN: 1616-301X- Author Web Link
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- Citations: 96
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Journal articleVilar R, 2004,
Hydrogen-bonding templated assemblies
, SUPRAMOLECULAR ASSEMBLY VIA HYDROGEN BONDS II, Vol: 111, Pages: 85-137, ISSN: 0081-5993- Author Web Link
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- Citations: 22
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Journal articleKrishnadasan S, Tovilla J, Vilar R, et al., 2004,
On-line analysis of CdSe nanoparticle formation in a continuous flow chip-based microreactor
, JOURNAL OF MATERIALS CHEMISTRY, Vol: 14, Pages: 2655-2660, ISSN: 0959-9428- Author Web Link
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- Citations: 122
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Journal articleOwen GR, Vilar R, White AJP, et al., 2003,
Studies on the reactivity of isocyanates and isothiocyanates with palladium-imidoyl complexes
, ORGANOMETALLICS, Vol: 22, Pages: 4511-4521, ISSN: 0276-7333- Author Web Link
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- Citations: 30
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Conference paperDoxiadi E, Vilar R, White AJP, et al., 2003,
Anion-templated synthesis and structural characterisation of Ni/Pd-containing metalla-macrocycles
, 223rd ACS National Meeting, Publisher: PERGAMON-ELSEVIER SCIENCE LTD, Pages: 2991-2998, ISSN: 0277-5387- Author Web Link
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- Citations: 38
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Journal articleOwen GR, Vilar R, White AJP, et al., 2003,
Synthesis and structural characterization of a novel dipalladium complex with an unprecedented PdCN bonding motif
, ORGANOMETALLICS, Vol: 22, Pages: 3025-3027, ISSN: 0276-7333- Author Web Link
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- Citations: 18
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Conference paperEdel JB, Krishmadasan S, Tovilla cao-Romero J, et al., 2003,
Continuous real-time monitoring of quantum dot synthesis within microfluidic reactors
, International conference on minaturized chemical and biochemical analysis systems; Micro total analysis systems 2003, Pages: 673-674 -
Journal articleVilar R, 2003,
Anion-templated synthesis
, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, Vol: 42, Pages: 1460-1477, ISSN: 1433-7851- Author Web Link
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- Citations: 337
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Journal articleWilliamson AM, Owen GR, Mingos DMP, et al., 2003,
Synthesis and structural characterisation of the palladium cluster compounds [Pd<sub>3</sub>(μ-SO<sub>2</sub>)<sub>2</sub>(μ-PPh<sub>2</sub>py)<sub>2</sub>(PBz<sub>3</sub>)<sub>2</sub>] and [Pd<sub>4</sub>(μ-SO<sub>2</sub>)<sub>2</sub>(μ<sub>3</sub>-S)(CNR)(PBz<sub>3</sub>)<sub>4</sub>] (R = <SUP>t</SUP>Bu, 2,6-dimethylphenyl and cyclohexyl)
, DALTON TRANSACTIONS, Pages: 2526-2532, ISSN: 1477-9226- Author Web Link
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- Citations: 6
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