Publications

Toxicology in Vitro

 Lipinski RJ, Bushman W
 Toxicology in Vitro - vol. 24 1404-1409 (2010)

In animal models, chemical disruption of the Hedgehog (Hh) signaling pathway during embryonic development causes severe birth defects including holoprosencephaly and cleft lip and palate. The exact etiological basis of correlate human birth defects remains uncertain but is likely multifactorial, involving the interaction of genetic and environmental or chemical influences. The Hh transduction mechanism relies […]

Leukemia Research

 Feng R, Rios JA, Onishi T, Lokshin A, Gorelik E, Lentzsch S
 Leukemia Research - vol. 34 917-924 (2010)

We used a novel high-throughput drug screening assay, based on Luminex technology, to identify anti-myeloma agents capable of inhibiting cytokines and growth factors essential for multiple myeloma (MM) from a chemical library of 1120 compounds provided by MMRF. Tetracycline derivatives inhibited MM cell proliferation and osteoclast activating factors without obvious effect on cell viability. Steroid […]

Stem Cell Research

 Barbaric I, Gokhale PJ, Jones M, Glen A, Baker D, Andrews PW
 Stem Cell Research - vol. 5 104-119 (2010)

Understanding the complex mechanisms that govern the fate decisions of human embryonic stem cells (hESCs) is fundamental to their use in cell replacement therapies. The progress of dissecting these mechanisms will be facilitated by the availability of robust high-throughput screening assays on hESCs. In this study, we report an image-based high-content assay for detecting compounds […]

Analytical Biochemistry

 Carme Mulero M, Orz??ez M, Messeguer J, Messeguer ?, P??rez-Pay?? E, P??rez-Riba M
 Analytical Biochemistry - vol. 398 99-103 (2010)

Calcineurin is a Ca2+/calmodulin-dependent serine/threonine protein phosphatase involved in many biological processes and developmental programs, including immune response. One of the most studied substrates of calcineurin is the transcription factor NFAT (nuclear factor of activated T cells) responsible for T-cell activation. Different anticalcineurin drugs, such as cyclosporine A and FK506, are the most commonly used […]

Applied Microbiology and Biotechnology

 Antoniani D, Bocci P, MacIa̧g A, Raffaelli N, Landini P
 Applied Microbiology and Biotechnology - vol. 85 1095-1104 (2010)

In Gram-negative bacteria, production of bis-(3′,5′)-cyclic diguanylic acid (c-di-GMP) by diguanylate cyclases (DGCs) is the main trigger for production of extracellular polysaccharides and for biofilm formation. Mutants affected in c-di-GMP biosynthesis are impaired in biofilm formation, thus making DGCs interesting targets for new antimicrobial agents with anti-biofilm activity. In this report, we describe a strategy […]

Current chemical genomics

 Gui C, Obaidat A, Chaguturu R, Hagenbuch B
 Current chemical genomics - vol. 4 1-8 (2010)

The two organic anion transporting polypeptides (OATPs) 1B1 and 1B3 are expressed at the sinusoidal membrane of hepatocytes. They have a broad and overlapping substrate specificity and transport many endobiotics and drugs. Specific inhibitors are required to determine the contribution of each OATP to the hepatocellular uptake of common substrates. We have developed a cell-based […]

The Journal of pharmacology and experimental therapeutics

 Doughty-Shenton D, Joseph JD, Zhang J, Pagliarini DJ, Kim Y, Lu D, Dixon JE, Casey PJ
 The Journal of pharmacology and experimental therapeutics - vol. 333 584-92 (2010)

The dual-specificity protein tyrosine phosphatases (PTPs) play integral roles in the regulation of cell signaling. There is a need for new tools to study these phosphatases, and the identification of inhibitors potentially affords not only new means for their study, but also possible therapeutics for the treatment of diseases caused by their dysregulation. However, the […]

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 […]

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