Search Results - "Leese, M P"

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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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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In vivo and in vitro properties of STX2484: a novel non-steroidal anti-cancer compound active in taxane-resistant breast cancer by Stengel, C, Newman, S P, Day, J M, Chander, S K, Jourdan, F L, Leese, M P, Ferrandis, E, Regis-Lydi, S, Potter, B V L, Reed, M J, Purohit, A, Foster, P A

“…Background: STX2484 is a novel non-steroidal compound with potent anti-proliferative activity. These studies aimed to identify STX2484’s mechanism of action,…”
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In vivo inhibition of angiogenesis by sulphamoylated derivatives of 2-methoxyoestradiol by CHANDER, S. K, FOSTER, P. A, LEESE, M. P, NEWMAN, S. P, POTTER, B. V. L, PUROHIT, A, REED, M. J

“…Drugs that inhibit growth of tumours and their blood supply could have considerable therapeutic potential. 2-Methoxyoestradiol-3,17-O,O-bis-sulphamate…”
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Steroid sulphatase inhibitors for breast cancer therapy by Purohit, A, Woo, L.W.L, Chander, S.K, Newman, S.P, Ireson, C, Ho, Y, Grasso, A, Leese, M.P, Potter, B.V.L, Reed, M.J

“…In contrast to aromatase inhibitors, which are now in clinical use, the development of steroid sulphatase (STS) inhibitors for breast cancer therapy is still…”
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BCRP expression does not result in resistance to STX140 in vivo, despite the increased expression of BCRP in A2780 cells in vitro after long-term STX140 exposure by Day, J M, Foster, P A, Tutill, H J, Newman, S P, Ho, Y T, Leese, M P, Potter, B V L, Reed, M J, Purohit, A

“…The anti-proliferative and anti-angiogenic properties of the endogenous oestrogen metabolite, 2-methoxyoestradiol (2-MeOE2), are enhanced in a series of…”
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The therapeutic potential of a series of orally bioavailable anti-angiogenic microtubule disruptors as therapy for hormone-independent prostate and breast cancers by NEWMAN, S. P, FOSTER, P. A, HO, Y. T, DAY, J. M, RAOBAIKADY, B, KASPRZYK, P. G, LEESE, M. P, POTTER, B. V. L, REED, M. J, PUROHIT, A

“…Therapies for hormone-independent prostate and breast cancer are limited, with the effectiveness of the taxanes compromised by toxicity, lack of oral…”
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The in vivo properties of STX243: a potent angiogenesis inhibitor in breast cancer by Parsons, M F C, Foster, P A, Chander, S K, Jhalli, R, Newman, S P, Leese, M P, Potter, B V L, Purohit, A, Reed, M J

“…The steroidal-based drug 2-ethyloestradiol-3,17- O , O - bis -sulphamate (STX243) has been developed as a potent antiangiogenic and antitumour compound. The…”
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Inhibition of carbonic anhydrase II by steroidal and non-steroidal sulphamates by Ho, Y.T., Purohit, A., Vicker, N., Newman, S.P., Robinson, J.J., Leese, M.P., Ganeshapillai, D., Woo, L.W.L., Potter, B.V.L., Reed, M.J.

“…Carbonic anhydrases (CAs) are expressed by many solid tumours where they may act to confer a growth advantage on malignant tissues. In this study we have…”
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Regulation of aromatase activity by cytokines, PGE2 and 2-methoxyoestrone-3- O-sulphamate in fibroblasts derived from normal and malignant breast tissues by Purohit, A., Ghilchik, M.W., Leese, M.P., Potter, B.V.L., Reed, M.J.

“…Synthesis of oestrone from androstenedione within tumours, by the aromatase enzyme complex, is an important source of oestrogen that is available to support…”
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The effects of 2-methoxyoestrogen sulphamates on the in vitro and in vivo proliferation of breast cancer cells by Utsumi, T., Leese, M.P., Chander, S.K., Gaukroger, K., Purohit, A., Newman, S.P., Potter, B.V.L., Reed, M.J.

“…2-Methoxyoestrogen sulphamates are a new class of compounds, which inhibit breast cancer cell proliferation and are also potent inhibitors of steroid…”
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Growth inhibition of multi-drug-resistant breast cancer cells by 2-methoxyoestradiol-bis-sulphamate and 2-ethyloestradiol-bis-sulphamate by Suzuki, R.N, Newman, S.P, Purohit, A, Leese, M.P, Potter, B.V.L, Reed, M.J

“…There is currently considerable interest in the use of the endogenous oestrogen metabolite, 2-methoxyoestradiol (2-MeOE2) for the treatment and prevention of…”
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The effects of 2-methoxy oestrogens and their sulphamoylated derivatives in conjunction with TNF-α on endothelial and fibroblast cell growth, morphology and apoptosis by Ho, Y.T., Newman, S.P., Purohit, A., Leese, M.P., Potter, B.V.L., Reed, M.J.

“…2-Methoxyoestradiol (2-MeOE2) is a potent anti-angiogenic agent. Its 3- and 17-sulphamoylated derivatives have been demonstrated to induce G 2-M cell cycle…”
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2-MeOE2bisMATE induces caspase-dependent apoptosis in CAL51 breast cancer cells and overcomes resistance to TRAIL via cooperative activation of caspases by Wood, L, Leese, M P, Mouzakiti, A, Purohit, A, Potter, B V L, Reed, M J, Packham, G

“…2-Methoxyoestradiol (2-MeOE2) is an endogenous oestrogen metabolite which inhibits tubulin polymerisation and has anti-tumour and anti-angiogenic activity…”
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2-Methoxyoestradiol-3,17-O,O-bis-sulphamate and 2-deoxy-D-glucose in combination: a potential treatment for breast and prostate cancer by Tagg, S L C, Foster, P A, Leese, M P, Potter, B V L, Reed, M J, Purohit, A, Newman, S P

“…Drug combination therapy is a key strategy to improve treatment efficacy and survival of cancer patients. In this study the effects of combining…”
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Anti-cancer activities of novel D-ring modified 2-substituted estrogen-3- O-sulfamates by Leese, Mathew P., Leblond, Bertrand, Newman, Simon P., Purohit, Atul, Reed, Michael J., Potter, Barry V.L.

“…Sulfamoylated derivatives of the endogenous estrogen metabolite 2-methoxyestradiol (2-MeOE2 ( 7)), such as 2-methoxy-3- O-sulfamoyl estrone (2-MeOEMATE ( 1)),…”
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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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Class III [beta]-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

“…Class III beta-tubulin overexpression is a marker of resistance to microtubule disruptors in vitro, in vivo and in the clinic for many cancers, including…”
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2-Methoxyoestradiol-3,17-O,O-his-sulphamate and 2-deoxy-D-glucose in combination : a potential treatment for breast and prostate cancer by TAGG, S. L. C, FOSTER, P. A, LEESE, M. P, POTTER, B. V. L, REED, M. J, PUROHIT, A, NEWMAN, S. P

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A New Micronized Formulation of 2-Methoxyestradiol-bis-sulfamate (STX140) is Therapeutically Potent against Breast Cancer by FOSTER, Paul A, NEWMAN, Simon P, REED, Michael J, PUROHIT, Atul, LEESE, Mathew P, BERNETIERE, Sonia, DIOLEZ, Christian, CAMARA, Jose, HACHER, Beatrice, BARONNET, Marie-Madeleine, ALI, Tauhid, POTTER, Barry V. L

“…There is a continued need for orally bioavailable anticancer compounds that exhibit good efficacy against breast cancer. STX140, a derivative of…”
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