Imperial College London

Dr Woscholski

Faculty of Natural SciencesDepartment of Chemistry

Reader in Chemical Biology
 
 
 
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Contact

 

+44 (0)20 7594 5305r.woscholski

 
 
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Location

 

6.22Flowers buildingSouth Kensington Campus

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Summary

 

Publications

Publication Type
Year
to

92 results found

Cilibrizzi A, Fedorova M, Collins J, Leatherbarrow R, Woscholski R, Vilar Ret al., 2017, A tri-functional vanadium(IV) complex to detect cysteine oxidation, DALTON TRANSACTIONS, Vol: 46, Pages: 6994-7004, ISSN: 1477-9226

JOURNAL ARTICLE

Cilibrizzi A, Terenghi M, Fedorova M, Woscholski R, Klug D, Vilar Ret al., 2017, Small-molecule optical probes for cell imaging of protein sulfenylation and their application to monitor cisplatin induced protein oxidation, SENSORS AND ACTUATORS B-CHEMICAL, Vol: 248, Pages: 437-446, ISSN: 0925-4005

JOURNAL ARTICLE

Billcliff PG, Noakes CJ, Mehta ZB, Yan G, Mak L, Woscholski R, Lowe Met al., 2016, OCRL1 engages with the F-BAR protein pacsin 2 to promote biogenesis of membrane-trafficking intermediates, MOLECULAR BIOLOGY OF THE CELL, Vol: 27, Pages: 90-107, ISSN: 1059-1524

JOURNAL ARTICLE

Collins J, Cilibrizzi A, Fedorova M, Whyte G, Mak LH, Guterman I, Leatherbarrow R, Woscholski R, Vilar Ret al., 2016, Vanadyl complexes with dansyl-labelled dipicolinic acid ligands: synthesis, phosphatase inhibition activity and cellular uptake studies, DALTON TRANSACTIONS, Vol: 45, Pages: 7104-7113, ISSN: 1477-9226

JOURNAL ARTICLE

Furse S, Brooks NJ, Woscholski R, Gaffney PRJ, Templer RHet al., 2016, Pressure-dependent inverse bicontinuous cubic phase formation in a phosphatidylinositol 4-phosphate/phosphatidylcholine system, Chemical Data Collections, Vol: 3-4, Pages: 15-20

© 2016 In this paper, we report the inositide-driven formation of an inverse bicontinuous cubic phase with space group Ia3d (Q II G , gyroid phase). The system under study consisted of distearoylphosphatidylinositol 4-phosphate (DSPIP) and dioleoylphosphatidylcholine at a molar ratio of 1:49, with a physiological concentration of magnesium ions at pH 7·4. The behaviour of the system was monitored as a function of temperature and pressure. The formation of the phase with Ia3d geometry was recorded repeatably at high pressure, and occurred more readily at higher temperatures. We conclude that the Ia3d phase formed is a thermodynamically stable structure, and that DSPIP is a potent source of membrane curvature that can drive the formation of mesophases with both 2- and 3D geometry.

JOURNAL ARTICLE

Verrastro I, Tveen-Jensen K, Woscholski R, Spickett CM, Pitt ARet al., 2016, Reversible oxidation of phosphatase and tensin homolog (PTEN) alters its interactions with signaling and regulatory proteins, FREE RADICAL BIOLOGY AND MEDICINE, Vol: 90, Pages: 24-34, ISSN: 0891-5849

JOURNAL ARTICLE

Wilson N, Mak LH, Cilibrizzi A, Gee AD, Long NJ, Woscholski R, Vilar Ret al., 2016, A lipophilic copper(II) complex as an optical probe for intracellular detection of NO, DALTON TRANSACTIONS, Vol: 45, Pages: 18177-18182, ISSN: 1477-9226

JOURNAL ARTICLE

Furse S, Mak L, Tate EW, Templer RH, Ces O, Woscholski R, Gaffney PRJet al., 2015, Synthesis of unsaturated phosphatidylinositol 4-phosphates and the effects of substrate unsaturation on SopB phosphatase activity, ORGANIC & BIOMOLECULAR CHEMISTRY, Vol: 13, Pages: 2001-2011, ISSN: 1477-0520

JOURNAL ARTICLE

Mak LH, Woscholski R, 2015, Targeting PTEN using small molecule inhibitors., Methods, Vol: 77-78C, Pages: 63-68, ISSN: 1046-2023

PTEN (phosphatase and tensin homologue deleted on chromosome 10) is well known as a tumour suppressor. It's PI(3,4,5)P3 lipid phosphatase activity is an important counteracting mechanism in PI 3-kinase (phosphoinositide 3-kinase) signalling. Furthermore, PTEN lies upstream of Akt kinase, a key enzyme in insulin signalling regulating glucose uptake and cell growth. Therefore, PTEN has recently gained attention as a valuable drug target for the treatment of diabetes, stroke, cardiac infarct and fertility. This review summarizes the use of small molecules as PTEN inhibitors. Currently available methodologies and techniques for accessing PTEN inhibition in vitro and in cellulo will be discussed.

JOURNAL ARTICLE

Murray JI, Woscholski R, Spivey AC, 2015, Organocatalytic Phosphorylation of Alcohols Using Pyridine-N-oxide, SYNLETT, Vol: 26, Pages: 985-990, ISSN: 0936-5214

JOURNAL ARTICLE

Amor B, Yaliraki SN, Woscholski R, Barahona Met al., 2014, Uncovering allosteric pathways in caspase-1 using Markov transient analysis and multiscale community detection, MOLECULAR BIOSYSTEMS, Vol: 10, Pages: 2247-2258, ISSN: 1742-206X

JOURNAL ARTICLE

Cilibrizzi A, Collins J, Woscholski R, Leatherbarrow R, Vilar Ret al., 2014, New vanadium complexes as optical probes to detect Cys sulfenic modifications in PTEN, 12th European Biological Inorganic Chemistry Conference (EuroBIC), Publisher: SPRINGER, Pages: S873-S873, ISSN: 0949-8257

CONFERENCE PAPER

Murray JI, Woscholski R, Spivey AC, 2014, Highly efficient and selective phosphorylation of amino acid derivatives and polyols catalysed by 2-aryl-4-(dimethylamino)pyridine-N-oxides - towards kinase-like reactivity, CHEMICAL COMMUNICATIONS, Vol: 50, Pages: 13608-13611, ISSN: 1359-7345

JOURNAL ARTICLE

O'Donnelly K, Zhao G, Patel P, Butt MS, Mak LH, Kretschmer S, Woscholski R, Barter LMCet al., 2014, Isolation and kinetic characterisation of hydrophobically distinct populations of form I Rubisco, PLANT METHODS, Vol: 10, ISSN: 1746-4811

JOURNAL ARTICLE

Pulido R, Baker SJ, Barata JT, Carracedo A, Cid VJ, Chin-Sang ID, Dave V, den Hertog J, Devreotes P, Eickholt BJ, Eng C, Furnari FB, Georgescu M-M, Gericke A, Hopkins B, Jiang X, Lee S-R, Loesche M, Malaney P, Matias-Guiu X, Molina M, Pandolfi PP, Parsons R, Pinton P, Rivas C, Rocha RM, Rodriguez MS, Ross AH, Serrano M, Stambolic V, Stiles B, Suzuki A, Tan S-S, Tonks NK, Trotman LC, Wolff N, Woscholski R, Wu H, Leslie NRet al., 2014, A Unified Nomenclature and Amino Acid Numbering for Human PTEN, SCIENCE SIGNALING, Vol: 7, ISSN: 1945-0877

JOURNAL ARTICLE

Woscholski R, 2014, Chemical intervention tools to probe phosphoinositide-dependent signalling, BIOCHEMICAL SOCIETY TRANSACTIONS, Vol: 42, Pages: 1343-1348, ISSN: 0300-5127

JOURNAL ARTICLE

Miller D, Booth PJ, Seddon JM, Templer RH, Law RV, Woscholski R, Ces O, Barter LMCet al., 2013, Protocell design through modular compartmentalization, JOURNAL OF THE ROYAL SOCIETY INTERFACE, Vol: 10, ISSN: 1742-5689

JOURNAL ARTICLE

Murray JI, Spivey AC, Woscholski R, 2013, Alternative synthetic tools to phospho-specific antibodies for phosphoproteome analysis: progress and prospects., J Chem Biol, Vol: 6, Pages: 175-184, ISSN: 1864-6158

Signal transduction cascades in living systems are often controlled via post-translational phosphorylation and dephosphorylation of proteins. These processes are catalyzed in vivo by kinase and phosphatase enzymes, which consequently play an important role in many disease states, including cancer and immune system disorders. Current techniques for studying the phosphoproteome (isotopic labeling, chromatographic techniques, and phosphospecific antibodies), although undoubtedly very powerful, have yet to provide a generic tool for phosphoproteomic analysis despite the widespread utility such a technique would have. The use of small molecule organic catalysts that can promote selective phosphate esterification could provide a useful alternative to current state-of-the-art techniques for use in, e.g., the labeling and pull-down of phosphorylated proteins. This report reviews current techniques used for phosphoproteomic analysis and the recent use of small molecule peptide-based catalysts in phosphorylation reactions, indicating possible future applications for this type of catalyst as synthetic alternatives to phosphospecific antibodies for phosphoproteome analysis.

JOURNAL ARTICLE

Whyte GF, Vilar R, Woscholski R, 2013, Molecular recognition with boronic acids-applications in chemical biology., J Chem Biol, Vol: 6, Pages: 161-174, ISSN: 1864-6158

Small molecules have long been used for the selective recognition of a wide range of analytes. The ability of these chemical receptors to recognise and bind to specific targets mimics certain biological processes (such as protein-substrate interactions) and has therefore attracted recent interest. Due to the abundance of biological molecules possessing polyhydroxy motifs, boronic acids-which form five-membered boronate esters with diols-have become increasingly popular in the synthesis of small chemical receptors. Their targets include biological materials and natural products including phosphatidylinositol bisphosphate, saccharides and polysaccharides, nucleic acids, metal ions and the neurotransmitter dopamine. This review will focus on the many ways in which small chemical receptors based on boronic acids have been used as biochemical tools for various purposes, including sensing and detection of analytes, interference in signalling pathways, enzyme inhibition and cell delivery systems. The most recent developments in each area will be highlighted.

JOURNAL ARTICLE

Charalambous K, Booth PJ, Woscholski R, Seddon JM, Templer RH, Law RV, Barter LMC, Ces Oet al., 2012, Engineering de Novo Membrane-Mediated Protein-Protein Communication Networks, JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Vol: 134, Pages: 5746-5749, ISSN: 0002-7863

JOURNAL ARTICLE

Domart M-C, Hobday TMC, Peddie CJ, Chung GHC, Wang A, Yeh K, Jethwa N, Zhang Q, Wakelam MJO, Woscholski R, Byrne RD, Collinson LM, Poccia DL, Larijani Bet al., 2012, Acute Manipulation of Diacylglycerol Reveals Roles in Nuclear Envelope Assembly & Endoplasmic Reticulum Morphology, PLOS ONE, Vol: 7, ISSN: 1932-6203

JOURNAL ARTICLE

Furse S, Brooks NJ, Seddon AM, Woscholski R, Templer RH, Tate EW, Gaffney PRJ, Ces Oet al., 2012, Lipid membrane curvature induced by distearoyl phosphatidylinositol 4-phosphate, SOFT MATTER, Vol: 8, Pages: 3090-3093, ISSN: 1744-683X

JOURNAL ARTICLE

Mak LH, Knott J, Scott KA, Scott C, Whyte GF, Ye Y, Mann DJ, Ces O, Stivers J, Woscholski Ret al., 2012, Arylstibonic acids are potent and isoform-selective inhibitors of Cdc25a and Cdc25b phosphatases, BIOORGANIC & MEDICINAL CHEMISTRY, Vol: 20, Pages: 4371-4376, ISSN: 0968-0896

JOURNAL ARTICLE

Wormit A, Butt SM, Chairam I, McKenna JF, Nunes-Nesi A, Kjaer L, O'Donnelly K, Fernie AR, Woscholski R, Barter MCL, Hamann Tet al., 2012, Osmosensitive Changes of Carbohydrate Metabolism in Response to Cellulose Biosynthesis Inhibition, PLANT PHYSIOLOGY, Vol: 159, Pages: 105-117, ISSN: 0032-0889

JOURNAL ARTICLE

Georgiades SN, Mak LH, Angurell I, Rosivatz E, Mustapa MFM, Polychroni C, Woscholski R, Vilar Ret al., 2011, Identification of a potent activator of Akt phosphorylation from a novel series of phenolic, picolinic, pyridino, and hydroxamic zinc(II) complexes, JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY, Vol: 16, Pages: 195-208, ISSN: 0949-8257

JOURNAL ARTICLE

Mak LH, Georgiades SN, Rosivatz E, Whyte GF, Mirabelli M, Vilar R, Woscholski Ret al., 2011, A Small Molecule Mimicking a Phosphatidylinositol (4,5)-Bisphosphate Binding Pleckstrin Homology Domain, ACS CHEMICAL BIOLOGY, Vol: 6, Pages: 1382-1390, ISSN: 1554-8929

JOURNAL ARTICLE

Rosivatz E, Woscholski R, 2011, Removal or masking of phosphatidylinositol(4,5)bisphosphate from the outer mitochondrial membrane causes mitochondrial fragmentation, CELLULAR SIGNALLING, Vol: 23, Pages: 478-486, ISSN: 0898-6568

JOURNAL ARTICLE

Alimonti A, Nardella C, Chen Z, Clohessy JG, Carracedo A, Trotman LC, Cheng K, Varmeh S, Kozma SC, Thomas G, Rosivatz E, Woscholski R, Cognetti F, Scher HI, Pandolfi PPet al., 2010, A novel type of cellular senescence that can be enhanced in mouse models and human tumor xenografts to suppress prostate tumorigenesis, JOURNAL OF CLINICAL INVESTIGATION, Vol: 120, Pages: 681-693, ISSN: 0021-9738

JOURNAL ARTICLE

Alimonti A, Nardella C, Pavese I, Clohessy JG, Carracedo A, Trotman LC, Woscholski R, Cognetti F, Scher HI, Pandolfi Pet al., 2010, PTEN and MDM2 inhibitors; Toward a novel pro-senescence therapy approach for patients with cancer., JOURNAL OF CLINICAL ONCOLOGY, Vol: 28, ISSN: 0732-183X

JOURNAL ARTICLE

Mak LH, Vilar R, Woscholski R, 2010, Characterisation of the PTEN inhibitor VO-OHpic., J Chem Biol, Vol: 3, Pages: 157-163

PTEN (phosphatase and tensin homologue deleted on chromosome 10) is a phosphatidylinositol triphosphate 3-phosphatase that counteracts phosphoinositide 3-kinases and has subsequently been implied as a valuable drug target for diabetes and cancer. Recently, we demonstrated that VO-OHpic is an extremely potent inhibitor of PTEN with nanomolar affinity in vitro and in vivo. Given the importance of this inhibitor for future drug design and development, its mode of action needed to be elucidated. It was discovered that inhibition of recombinant PTEN by VO-OHpic is fully reversible. Both K(m) and V(max) are affected by VO-OHpic, demonstrating a noncompetitive inhibition of PTEN. The inhibition constants K(ic) and K(iu) were determined to be 27 ± 6 and 45 ± 11 nM, respectively. Using the artificial phosphatase substrate 3-O-methylfluorescein phosphate (OMFP) or the physiological substrate phosphatidylinositol 3,4,5-triphosphate (PIP(3)) comparable parameters were obtained suggesting that OMFP is a suitable substrate for PTEN inhibition studies and PTEN drug screening.

JOURNAL ARTICLE

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