Publications

Neuropharmacology

 Buckley CE, Marguerie A, Roach AG, Goldsmith P, Fleming A, Alderton WK, Franklin RJM
 Neuropharmacology - vol. 59 149-159 (2010)

Treatment of the autoimmune demyelinating disease multiple sclerosis (MS) requires therapies that both limit and repair damage. While several immunomodulatory treatments exist to limit damage there are currently no treatments that promote the regenerative process of remyelination. A rapid way of screening potential pro-remyelination compounds is therefore required. The use of larval zebrafish in a […]

Journal of biomolecular screening

 Dearmond PD, West GM, Anbalagan V, Campa MJ, Patz EF, Fitzgerald MC
 Journal of biomolecular screening - vol. 15 1051-62 (2010)

Cyclophilin A (CypA) is an overexpressed protein in lung cancer tumors and as a result is a potential therapeutic and diagnostic target. Described here is use of an H/D exchange- and a matrix assisted laser desorption/ionization (MALDI) mass spectrometry-based assay, termed single-point SUPREX (Stability of Unpurified Proteins from Rates of H/D Exchange), to screen 2 […]

The Biochemical journal

 Andrews PD, Becroft M, Aspegren A, Gilmour J, James MJ, McRae S, Kime R, Allcock RW, Abraham A, Jiang Z, Strehl R, Mountford JC, Milligan G, Houslay MD, Adams DR, Frearson JA, Watanabe K, Ueno M, Kamiya D, Nishiyama A, Matsumura M, Wataya T, Takahashi J, Nishikawa S, Nishikawa S, Muguruma K, Sasai Y, Claassen D, Desler M, Rizzino A, Li X, Meng G, Krawetz R, Liu S, Rancourt D, Krawetz R, Li X, Rancourt D, Olson M, Davies S, Reddy H, Caivano M, Cohen P, Darenfed H, Dayanandan B, Zhang T, Hsieh S, Fournier A, Mandato C, Liu Y, Song Z, Zhao Y, Qin H, Cai J, Zhang H, Yu T, Jiang S, Wang G, Ding M, Deng H, Brenk R, Schipani A, James D, Krasowski A, Gilbert I, Frearson J, Wyatt P, Zhang J, Chung T, Oldenburg K, Grover G, Nichols R, Dzamko N, Hutti J, Cantley L, Deak M, Moran J, Bamborough P, Reith A, Alessi D, Takami A, Iwakubo M, Okada Y, Kawata T, Odai H, Takahashi N, Shindo K, Kimura K, Tagami Y, Miyake M, Yamaguchi H, Miwa Y, Kasa M, Kitano K, Amano M, Kaibuchi K, Hakoshima T, Jacobs M, Hayakawa K, Swenson L, Bellon S, Fleming M, Taslimi P, Doran J, Yamaguchi H, Kasa M, Amano M, Kaibuchi K, Hakoshima T, Iwakubo M, Takami A, Okada Y, Kawata T, Tagami Y, Ohashi H, Sato M, Sugiyama T, Fukushima K, Iijima H, Mohammadi M, McMahon G, Sun L, Tang C, Hirth P, Yeh B, Hubbard S, Schlessinger J, Ardehali H, O'Rourke B, Laflamme M, Chen K, Naumova A, Muskheli V, Fugate J, Dupras S, Reinecke H, Xu C, Hassanipour M, Police S, Pasquale E, Wang X, Lin G, Martins-Taylor K, Zeng H, Xu R, Xu Y, Zhu X, Hahm H, Wei W, Hao E, Hayek A, Ding S, Vallier L, Alexander M, Pedersen R, Annerén C, Cowan C, Melton D, Meyn M, Schreiner S, Dumitrescu T, Nau G, Smithgall T, Barbaric I, Gokhale P, Jones M, Glen A, Baker D, Andrews P
 The Biochemical journal - vol. 432 21-33 (2010)

The propensity of human embryonic stem cells to die upon enzymatic disaggregation or low-density plating is an obstacle to their isolation and routine use in drug discovery and basic research. Equally, the very low rate of establishment of implanted cells hinders cell therapy. In the present study we have developed a high-content assay for human […]

Bioorganic and Medicinal Chemistry

 Kuhn I, Kellenberger E, Said-Hassane F, Villa P, Rognan D, Lobstein A, Haiech J, Hibert M, Schuber F, Muller-Steffner H
 Bioorganic and Medicinal Chemistry - vol. 18 7900-7910 (2010)

Schistosomiasis is a major tropical parasitic disease. For its treatment, praziquantel remains the only effective drug available and the dependence on this sole chemotherapy emphasizes the urgent need for new drugs to control this neglected disease. In this context, the newly characterized Schistosoma mansoni NAD+ catabolizing enzyme (SmNACE) represents a potentially attractive drug target. This […]

Molecular Informatics

 Langer T
 Molecular Informatics - vol. 29 470-475 (2010)

The pharmacophore concept in modern drug research is highlighted and the most important use examples and success stories are reviewed. These include papers from method development as well as from application areas. As indicated by the number of publications available, the pharmacophore approach has proven to be extremely useful as interface between medicinal and computational […]

Publications
Tuberculosis

 Manuscript A, Leads PD
 Tuberculosis - vol. 89 331-333 (2010)

Journal of biomolecular screening

 Haynes MK, Strouse JJ, Waller A, Leitao A, Curpan RF, Bologa C, Oprea TI, Prossnitz ER, Edwards BS, Sklar LA, Thompson TA
 Journal of biomolecular screening - vol. 14 596-609 (2009)

Prostate cancer is a leading cause of death among men due to the limited number of treatment strategies available for advanced disease. Discovery of effective chemotherapeutics involves the identification of agents that inhibit cancer cell growth. Increases in intracellular granularity have been observed during physiological processes that include senescence, apoptosis, and autophagy, making this phenotypic […]

Bioorganic and Medicinal Chemistry

 Zhu PJ, Hobson JP, Southall N, Qiu C, Thomas CJ, Lu J, Inglese J, Zheng W, Leppla SH, Bugge TH, Austin CP, Liu S
 Bioorganic and Medicinal Chemistry - vol. 17 5139-5145 (2009)

Here, we report the results of a quantitative high-throughput screen (qHTS) measuring the endocytosis and translocation of a β-lactamase-fused-lethal factor and the identification of small molecules capable of obstructing the process of anthrax toxin internalization. Several small molecules protect RAW264.7 macrophages and CHO cells from anthrax lethal toxin and protected cells from an LF-Pseudomonas exotoxin […]

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