Publications

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 […]

Current chemical genomics

 Larsen RS, Zylka MJ, Scott JE
 Current chemical genomics - vol. 3 42-9 (2009)

Prostatic acid phosphatase (PAP) is expressed in nociceptive neurons and functions as an ectonucleotidase. Injection of the secretory isoform of PAP has potent antinociceptive effects in mouse models of chronic pain. These data suggested that a small molecule activator of PAP may have utility as a novel therapeutic for chronic pain, while inhibitors could be […]

PLoS ONE

 Dubreuil P, Letard S, Ciufolini M, Gros L, Humbert M, Castéran N, Borge L, Hajem B, Lermet A, Sippl W, Voisset E, Arock M, Auclair C, Leventhal PS, Mansfield CD, Moussy A, Hermine O
 PLoS ONE - vol. 4 (2009)

BACKGROUND: The stem cell factor receptor, KIT, is a target for the treatment of cancer, mastocytosis, and inflammatory diseases. Here, we characterise the in vitro and in vivo profiles of masitinib (AB1010), a novel phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT.nnMETHODOLOGY/PRINCIPAL FINDINGS: In vitro, masitinib had greater activity and selectivity against KIT than imatinib, inhibiting […]

The Journal of experimental medicine

 Du L, Damoiseaux R, Nahas S, Gao K, Hu H, Pollard JM, Goldstine J, Jung ME, Henning SM, Bertoni C, Gatti RA
 The Journal of experimental medicine - vol. 206 2285-2297 (2009)

Large numbers of genetic disorders are caused by nonsense mutations for which compound-induced readthrough of premature termination codons (PTCs) might be exploited as a potential treatment strategy. We have successfully developed a sensitive and quantitative high-throughput screening (HTS) assay, protein transcription/translation (PTT)-enzyme-linked immunosorbent assay (ELISA), for identifying novel PTC-readthrough compounds using ataxia-telangiectasia (A-T) as a […]

PLoS Pathogens

 Charpentier X, Gabay JE, Reyes M, Zhu JW, Weiss A, Shuman HA
 PLoS Pathogens - vol. 5 (2009)

Delivery of effector proteins is a process widely used by bacterial pathogens to subvert host cell functions and cause disease. Effector delivery is achieved by elaborate injection devices and can often be triggered by environmental stimuli. However, effector export by the L. pneumophila Icm/Dot Type IVB secretion system cannot be detected until the bacterium encounters […]

Chemistry and Biology

 D'Elia MA, Millar KE, Bhavsar AP, Tomljenovic AM, Hutter B, Schaab C, Moreno-Hagelsieb G, Brown ED
 Chemistry and Biology - vol. 16 548-556 (2009)

The bacterial cell wall has been a celebrated target for antibiotics and holds real promise for the discovery of new antibacterial chemical matter. In addition to peptidoglycan, the walls of Gram-positive bacteria contain large amounts of the polymer teichoic acid, covalently attached to peptidoglycan. Recently, wall teichoic acid was shown to be essential to the […]

Trends in Pharmacological Sciences

 Conn PJ, Jones CK, Lindsley CW
 Trends in Pharmacological Sciences - vol. 30 148-155 (2009)

Muscarinic acetylcholine receptors (mAChRs) have long been viewed as viable targets for novel therapeutic agents for the treatment of Alzheimer’s disease (AD) and other disorders involving impaired cognitive function. More recent evidence indicates that mAChR activators might also have utility in treating psychosis and other symptoms associated with schizophrenia and other central nervous system (CNS) […]

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