Publications

Journal of biomolecular screening

 Norton JT, Titus SA, Dexter D, Austin CP, Zheng W, Huang S
 Journal of biomolecular screening - vol. 14 1045-1053 (2009)

All solid malignancies share characteristic traits, including unlimited cellular proliferation, evasion of immune regulation, and the propensity to metastasize. The authors have previously described that a subnuclear structure, the perinucleolar compartment (PNC), is associated with the metastatic phenotype in solid tumor cancer cells. The percentage of cancer cells that contain PNCs (PNC prevalence) is indicative […]

Current Opinion in Pharmacology

 Langer T, Hoffmann R, Bryant S, Lesur B
 Current Opinion in Pharmacology - vol. 9 589-593 (2009)

Drug discovery is complex and risky, and the chances of success are low. One starting point to discover a new drug is the selective screening of a collection of high value and good quality compounds. Selection of compounds for screening is one of the challenging initial steps in the drug discovery process and is crucial […]

Journal of Biological Chemistry

 Journal of Biological Chemistry - vol. 284 9394-9401 (2009)

Calcineurin phosphatase plays a crucial role in T cell activation. Dephosphorylation of the nuclear factors of activated T cells (NFATs) by calcineurin is essential for activating cytokine gene expression and, consequently, the immune response. Current immunosuppressive protocols are based mainly on calcineurin inhibitors, cyclosporine A and FK506. Unfortunately, these drugs are associated with severe side […]

Www.Sbsonline.Org

 MacArthur R, Leister W, Veith H, Shinn P, Southall N, Austin CP, Inglese J, Auld DS
 Www.Sbsonline.Org 1-9 (2009)

The authors describe how room temperature storage of a 1120-member compound library prepard in either DMSO or in a hydrated-DMSO/water (67/33) mixture affects the reproducibility of potency values as monitored using cytochrome P450 1A2 and 2D6 isozyme assays. The bioluminescent assays showed Z’factors of 0.71 and 0.62, with 17% and 32% of the library found […]

The Biochemical journal

 Iorns E, Lord CJ, Ashworth A
 The Biochemical journal - vol. 417 361-370 (2009)

Tamoxifen is the most commonly used drug to treat breast cancer and acts by blocking ERalpha (oestrogen receptor alpha) signalling. Although highly effective, its usefulness is limited by the development of resistance. Given this, strategies that limit resistance by sensitizing cells to tamoxifen may be of use in the clinic. To gain insight into how […]

Molecular Pharmacology

 Huang X, Setola V, Yadav PN, Allen JA, Rogan SC, Hanson BJ, Revankar C, Robers M, Doucette C, Roth BL
 Molecular Pharmacology - vol. 5 710-722 (2009)

Drug-induced valvular heart disease (VHD) is a serious side effect of a few medications, including some that are on the market. Pharmacological studies of VHD-associated medications (e.g., fenfluramine, pergolide, methysergide, and cabergoline) have revealed that they and/or their metabolites are potent 5-hydroxytryptamine2B (5-HT2B) receptor agonists. We have shown that activation of 5-HT2B receptors on human […]

PLoS Pathogens

 Pyeon D, Pearce SM, Lank SM, Ahlquist P, Lambert PF
 PLoS Pathogens - vol. 5 (2009)

Human papillomaviruses (HPVs) are DNA viruses associated with major human cancers. As such there is a strong interest in developing new means, such as vaccines and microbicides, to prevent HPV infections. Developing the latter requires a better understanding of the infectious life cycle of HPVs. The HPV infectious life cycle is closely linked to the […]

PLoS ONE

 Perne A, Muellner MK, Steinrueck M, Craig-Mueller N, Mayerhofer J, Schwarzinger I, Sloane M, Uras IZ, Hoermann G, Nijman SMB, Mayerhofer M
 PLoS ONE - vol. 4 (2009)

BACKGROUND: Cardiac glycosides are Na(+)/K(+)-pump inhibitors widely used to treat heart failure. They are also highly cytotoxic, and studies have suggested specific anti-tumor activity leading to current clinical trials in cancer patients. However, a definitive demonstration of this putative anti-cancer activity and the underlying molecular mechanism has remained elusive.nnMETHODOLOGY/PRINCIPAL FINDINGS: Using an unbiased transcriptomics approach, […]

Chemistry and Biology

 Livingstone M, Larsson O, Sukarieh R, Pelletier J, Sonenberg N
 Chemistry and Biology - vol. 16 1240-1249 (2009)

The signal transduction pathway wherein mTOR regulates cellular growth and proliferation is an active target for drug discovery. The search for new mTOR inhibitors has recently yielded a handful of promising compounds that hold therapeutic potential. This search has been limited by the lack of??a high-throughput assay to monitor the phosphorylation of a direct rapamycin-sensitive […]

BMC microbiology

 Kemmer D, McHardy LM, Hoon S, Rebérioux D, Giaever G, Nislow C, Roskelley CD, Roberge M
 BMC microbiology - vol. 9 9 (2009)

BACKGROUND: Single genome-wide screens for the effect of altered gene dosage on drug sensitivity in the model organism Saccharomyces cerevisiae provide only a partial picture of the mechanism of action of a drug.nnRESULTS: Using the example of the tumor cell invasion inhibitor dihydromotuporamine C, we show that a more complete picture of drug action can […]

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