Publications


Publications
Development of a cell-based high-throughput assay to screen for inhibitors of organic anion transporting polypeptides 1B1 and 1B3.

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 […]

Publications
High-content assay to identify inhibitors of dengue virus infection.

Assay and drug development technologies

Shum D, Smith JL, Hirsch AJ, Bhinder B, Radu C, Stein DA, Nelson JA, Früh K, Djaballah H
Assay and drug development technologies - vol. 8 553-70 (2010)

Dengue virus (DENV) infections are vectored by mosquitoes and constitute one of the most prevalent infectious diseases in many parts of the world, affecting millions of people annually. Current treatments for DENV infections are nonspecific and largely ineffective. In this study, we describe the adaptation of a high-content cell-based assay for screening against DENV-infected cells […]

Publications
Pharmacological targeting of the mitochondrial phosphatase PTPMT1.

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 […]

Publications
Modeling Liver-Related Adverse Effects of Drugs Using k Nearest Neighbor Quantitative Structure – Activity Relationship Method

Chemical research in toxicology

Rodgers AD, Zhu H, Fourches D, Rusyn I, Tropsha A, Hill C, Carolina N
Chemical research in toxicology - vol. 23 724-732 (2010)

Adverse effects of drugs (AEDs) continue to be a major cause of drug withdrawals in both development and postmarketing. While liver-related AEDs are a major concern for drug safety, there are few in silico models for predicting human liver toxicity for drug candidates. We have applied the quantitative structure-activity relationship (QSAR) approach tomodel liver AEDs. […]

Publications
Drug reprofiling using zebrafish identifies novel compounds with potential pro-myelination effects

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 […]

Publications
NIH Public Access

Manuscript A, Syndromes GP
- vol. 48 1-6 (2010)

Publications
Discovery of novel cyclophilin A ligands using an H/D exchange- and mass spectrometry-based strategy.

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 […]

Publications
Advances in flow cytometry for drug screening

Expert opinion on drug discovery

Peluso J, Muller CD
Expert opinion on drug discovery - vol. 5 827-833 (2010)

Importance of the field: Flow cytometry is considered today as a mature technology. Recently, it has become an accurate tool for screening applications. Yet, not many studies have been published emphasizing flow cytometry as a tool of choice for drug screening except multiplex bead assay. Areas covered in this review: Scanning the literature for technology […]

Publications
High-content screening of feeder-free human embryonic stem cells to identify pro-survival small molecules.

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 […]

Publications
Rapid behavior-based identification of neuroactive small molecules in the zebrafish

Nat Chem Biol

Kokel D, Bryan J, Laggner C, White R, Cheung CY, Mateus R, Healey D, Kim S, Werdich AA, Haggarty SJ, Macrae CA, Shoichet B, Peterson RT
Nat Chem Biol - vol. 6 231-237 (2010)

Neuroactive small molecules are indispensable tools for treating mental illnesses and dissecting nervous system function. However, it has been difficult to discover novel neuroactive drugs. Here, we describe a high-throughput, behavior-based approach to neuroactive small molecule discovery in the zebrafish. We used automated screening assays to evaluate thousands of chemical compounds and found that diverse […]