92 results found
Cilibrizzi A, Fedorova M, Collins J, et al., 2017, A tri-functional vanadium(IV) complex to detect cysteine oxidation, DALTON TRANSACTIONS, Vol: 46, Pages: 6994-7004, ISSN: 1477-9226
Cilibrizzi A, Terenghi M, Fedorova M, et 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
Billcliff PG, Noakes CJ, Mehta ZB, et 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
Collins J, Cilibrizzi A, Fedorova M, et 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
Furse S, Brooks NJ, Woscholski R, et 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.
Verrastro I, Tveen-Jensen K, Woscholski R, et 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
Wilson N, Mak LH, Cilibrizzi A, et 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
Furse S, Mak L, Tate EW, et 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
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.
Murray JI, Woscholski R, Spivey AC, 2015, Organocatalytic Phosphorylation of Alcohols Using Pyridine-N-oxide, SYNLETT, Vol: 26, Pages: 985-990, ISSN: 0936-5214
Amor B, Yaliraki SN, Woscholski R, et 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
Cilibrizzi A, Collins J, Woscholski R, et 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
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
O'Donnelly K, Zhao G, Patel P, et al., 2014, Isolation and kinetic characterisation of hydrophobically distinct populations of form I Rubisco, PLANT METHODS, Vol: 10, ISSN: 1746-4811
Pulido R, Baker SJ, Barata JT, et al., 2014, A Unified Nomenclature and Amino Acid Numbering for Human PTEN, SCIENCE SIGNALING, Vol: 7, ISSN: 1945-0877
Woscholski R, 2014, Chemical intervention tools to probe phosphoinositide-dependent signalling, BIOCHEMICAL SOCIETY TRANSACTIONS, Vol: 42, Pages: 1343-1348, ISSN: 0300-5127
Miller D, Booth PJ, Seddon JM, et al., 2013, Protocell design through modular compartmentalization, JOURNAL OF THE ROYAL SOCIETY INTERFACE, Vol: 10, ISSN: 1742-5689
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.
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.
Charalambous K, Booth PJ, Woscholski R, et 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
Domart M-C, Hobday TMC, Peddie CJ, et al., 2012, Acute Manipulation of Diacylglycerol Reveals Roles in Nuclear Envelope Assembly & Endoplasmic Reticulum Morphology, PLOS ONE, Vol: 7, ISSN: 1932-6203
Furse S, Brooks NJ, Seddon AM, et al., 2012, Lipid membrane curvature induced by distearoyl phosphatidylinositol 4-phosphate, SOFT MATTER, Vol: 8, Pages: 3090-3093, ISSN: 1744-683X
Mak LH, Knott J, Scott KA, et 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
Wormit A, Butt SM, Chairam I, et al., 2012, Osmosensitive Changes of Carbohydrate Metabolism in Response to Cellulose Biosynthesis Inhibition, PLANT PHYSIOLOGY, Vol: 159, Pages: 105-117, ISSN: 0032-0889
Georgiades SN, Mak LH, Angurell I, et 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
Mak LH, Georgiades SN, Rosivatz E, et 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
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
Alimonti A, Nardella C, Chen Z, et 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
Alimonti A, Nardella C, Pavese I, et 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
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.
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