Search Results - "Potter, BVL"

D-Ring Modified Estrone Derivatives as Novel Potent Inhibitors of Steroid Sulfatase by Fischer, Delphine S, Woo, L.W.Lawrence, Mahon, Mary F, Purohit, Atul, Reed, Michael J, Potter, Barry V.L

“…A series of novel D-ring modified derivatives of estrone was synthesized and tested as inhibitors of steroid sulfatase (STS). The steroidal D-ring was cleaved…”
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Differential effects of estrone and estrone-3-O-sulfamate derivatives on mitotic arrest, apoptosis, and microtubule assembly in human breast cancer cells by MACCARTHY-MORROGH, Lucy, TOWNSEND, Paul A, PUROHIT, Atul, HEJAZ, Hatem A. M, POTTER, Barry V. L, REED, Michael J, PACKHAM, Graham

“…There is considerable interest in the potential use of estrogen derivatives for the treatment and prevention of breast cancer. We demonstrated previously that…”
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Xylopyranoside-based agonists of d- myo-inositol 1,4,5-trisphosphate receptors: synthesis and effect of stereochemistry on biological activity by Rosenberg, Heidi J., Riley, Andrew M., Marwood, Rachel D., Correa, Vanessa, Taylor, Colin W., Potter, Barry V.L.

“…The synthesis of a series of tetrahydrofuranyl α- and β-xylopyranoside trisphosphates, designed by excision of three motifs of adenophostin A is reported. The…”
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Class III β-tubulin expression and in vitro resistance to microtubule targeting agents by Stengel, C, Newman, S P, Leese, M P, Potter, B V L, Reed, M J, Purohit, A

“…Background: Class III β -tubulin overexpression is a marker of resistance to microtubule disruptors in vitro , in vivo and in the clinic for many cancers,…”
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Steroid Sulfatase: Molecular Biology, Regulation, and Inhibition by Reed, M. J, Purohit, A, Woo, L. W. L, Newman, S. P, Potter, B. V. L

“…Steroid sulfatase (STS) is responsible for the hydrolysis of aryl and alkyl steroid sulfates and therefore has a pivotal role in regulating the formation of…”
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Phase I Study of STX 64 (667 Coumate) in Breast Cancer Patients: The First Study of a Steroid Sulfatase Inhibitor by STANWAY, Susannah J, PUROHIT, Atul, ELLIOTT, Moira, POTTER, Barry V. L, REED, Michael J, COOMBES, R. Charles, WOO, L. W. Lawrence, SUFI, Saulat, VIGUSHIN, David, WARD, Rebecca, WILSON, Richard H, STANCZYK, Frank Z, DOBBS, Nicola, KULINSKAYA, Elena

“…Purpose: Inhibition of steroid sulfatase (STS), the enzyme responsible for the hydrolysis of steroid sulfates, represents a potential novel treatment for…”
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Crystal Structures of Type-II Inositol Polyphosphate 5‑Phosphatase INPP5B with Synthetic Inositol Polyphosphate Surrogates Reveal New Mechanistic Insights for the Inositol 5‑Phosphatase Family by Mills, Stephen J, Silvander, Camilla, Cozier, Gyles, Trésaugues, Lionel, Nordlund, Pär, Potter, Barry V. L

“…The inositol polyphosphate 5-phosphatase INPP5B hydrolyzes the 5-phosphate group from water- and lipid-soluble signaling messengers. Two synthetic benzene and…”
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2-Substituted Estradiol Bis-sulfamates, Multitargeted Antitumor Agents:  Synthesis, In Vitro SAR, Protein Crystallography, and In Vivo Activity by Leese, Mathew P, Leblond, Bertrand, Smith, Andrew, Newman, Simon P, Di Fiore, Anna, De Simone, Giuseppina, Supuran, Claudiu T, Purohit, Atul, Reed, Michael J, Potter, Barry V. L

“…The anticancer activities and SARs of estradiol-17-O-sulfamates and estradiol 3,17-O,O-bis-sulfamates (E2bisMATEs) as steroid sulfatase (STS) inhibitors and…”
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Inhibition of the phosphatidylinositol 3-kinase/akt pathway by inositol pentakisphosphate results in antiangiogenic and antitumor effects by MAFFUCCI, Tania, PICCOLO, Enza, POTTER, Barry V. L, INNOCENTI, Paolo, FALASCA, Marco, CUMASHI, Albana, IEZZI, Manuela, RILEY, Andrew M, SAIARDI, Adolfo, GODAGE, H. Yasmin, ROSSI, Cosmo, BROGGINI, Massimo, IACOBELLI, Stefano

“…The purpose of this study was to investigate the antiangiogenic and in vivo properties of the recently identified phosphatidylinositol 3-kinase (PI3K)/Akt…”
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Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with EMATE, a dual inhibitor of carbonic anhydrases and steroid sulfatase by Abbate, Francesco, Winum, Jean-Yves, Potter, Barry V.L., Casini, Angela, Montero, Jean-Louis, Scozzafava, Andrea, Supuran, Claudiu T.

“…The X-ray crystal structure for the adduct of human carbonic anhydrase II (hCA II) with estrone-3- O-sulfamate (EMATE), an antiendocrine agent showing both CA…”
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A synthetic diphosphoinositol phosphate analogue of inositol trisphosphate by Riley, Andrew M, Unterlass, Judith, Konieczny, Vera, Taylor, Colin W, Helleday, Thomas, Potter, Barry V L

“…Diphosphoinositol phosphates (PP-InsPs) are inositol phosphates (InsPs) that contain PP (diphosphate) groups. Converting a phosphate group in an InsP into a…”
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Modes of cell death induced by tetrahydroisoquinoline-based analogs in MDA-MB-231 breast and A549 lung cancer cell lines by Nel, Marcel, Joubert, Anna M, Dohle, Wolfgang, Potter, Barry Vl, Theron, Anne E

“…A and B rings of the steroidal microtubule disruptor, 2-methoxyestradiol, and its analogs can be mimicked with a tetrahydroisoquinoline (THIQ) core. THIQs are…”
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A novel and selective PDK1 inhibitor reduces breast cancer cell invasion and tumour growth by Raimondi, C, Maffucci, T, Potter, BVL, Falasca, M

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A Synthetic Polyphosphoinositide Headgroup Surrogate in Complex with SHIP2 Provides a Rationale for Drug Discovery by Mills, Stephen J, Persson, Camilla, Cozier, Gyles, Thomas, Mark P, Trésaugues, Lionel, Erneux, Christophe, Riley, Andrew M, Nordlund, Pär, Potter, Barry V. L

“…Phosphoinositides regulate many cellular processes, and cellular levels are controlled by kinases and phosphatases. SHIP2 (SH2 (Src homology…”
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Identification of Mammalian Vps24p as an Effector of Phosphatidylinositol 3,5-Bisphosphate-dependent Endosome Compartmentalization by Whitley, Paul, Reaves, Barbara J., Hashimoto, Makoto, Riley, Andrew M., Potter, Barry V.L., Holman, Geoffrey D.

“…Phosphatidylinositol 3,5-bisphosphate is a membrane lipid found in all eukaryotes so far studied but downstream effector proteins of this lipid have yet to be…”
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Characterisation of the binding of [3H]methyllycaconitine: a new radioligand for labelling alpha 7-type neuronal nicotinic acetylcholine receptors by Davies, A R, Hardick, D J, Blagbrough, I S, Potter, B V, Wolstenholme, A J, Wonnacott, S

“…Methyllycaconitine (MLA), a norditerpenoid alkaloid isolated from Delphinium seeds, is one of the most potent non-proteinacious ligands that is selective for…”
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Benzothiazole derivatives as novel inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 by Su, Xiangdong, Vicker, Nigel, Ganeshapillai, Dharshini, Smith, Andrew, Purohit, Atul, Reed, Michael J., Potter, Barry V.L.

“…Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential as treatments for metabolic diseases, such as diabetes…”
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Nicotinic Acid Adenine Dinucleotide Phosphate (NAADP+) Is an Essential Regulator of T-Lymphocyte Ca2+-Signaling by Berg, Ingeborg, Barry V. L. Potter, Mayr, Georg W., Guse, Andreas H.

“…Microinjection of human Jurkat T-lymphocytes with nicotinic acid adenine dinucleotide phosphate (NAADP+) dose-dependently stimulated intracellular…”
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Pharmacokinetics and efficacy of 2-methoxyoestradiol and 2-methoxyoestradiol-bis-sulphamate in vivo in rodents by IRESON, C. R, CHANDER, S. K, PUROHIT, A, PERERA, S, NEWMAN, S. P, PARISH, D, LEESE, M. P, SMITH, A. C, POTTER, B. V. L, REED, M. J

“…2-Methoxyoestradiol (2-MeOE2) is an endogenous oestrogen metabolite that inhibits the proliferation of cancer cells in vitro, and it is also antiangiogenic. In…”
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Inhibition of steroid sulphatase activity in endometriotic implants by 667 COUMATE: a potential new therapy by Purohit, A., Fusi, L., Brosens, J., Woo, L.W.L., Potter, B.V.L., Reed, M.J.

“…BACKGROUND Local biosynthesis of estrogens is thought to be important for the maintenance and growth of endometriotic implants. In addition to the formation of…”
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