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Success Stories


Publications
Luteolin is a novel p90 ribosomal S6 kinase (RSK) inhibitor that suppresses Notch4 signaling by blocking the activation of Y-box binding protein-1 (YB-1).

Oncotarget

Reipas KM, Law JH, Couto N, Islam S, Li Y, Li H, Cherkasov A, Jung K, Cheema AS, Jones SJM, Hassell JA, Dunn SE
Oncotarget - vol. 4 329-345 (2013)

Triple-negative breast cancers (TNBC) are notoriously difficult to treat because they lack hormone receptors and have limited targeted therapies. Recently, we demonstrated that p90 ribosomal S6 kinase (RSK) is essential for TNBC growth and survival indicating it as a target for therapeutic development. RSK phosphorylates Y-box binding protein-1 (YB-1), an oncogenic transcription/translation factor, highly expressed […]

Publications
Novel surface-based methodologies for investigating GH11 xylanase-lignin derivative interactions.

The Analyst

Zeder-Lutz G, Renau-Ferrer S, Aguié-Béghin V, Rakotoarivonina H, Chabbert B, Altschuh D, Rémond C
The Analyst - vol. 138 6889-99 (2013)

The recalcitrance of lignocellulose to bioprocessing represents the core problem and remains the limiting factor in creating an economy based on lignocellulosic ethanol production. Lignin is responsible for unproductive interactions with enzymes, and understanding how lignin impairs the susceptibility of biomass to enzymatic hydrolysis represents a significant aim in optimising the biological deconstruction of lignocellulose. […]

Publications
Synergy of the antibiotic colistin with echinocandin antifungals in candida species

Journal of Antimicrobial Chemotherapy

Zeidler U, Bougnoux ME, Lupan A, Helynck O, Doyen A, Garcia Z, Sertour N, Clavaud C, Munier-Lehmann H, Saveanu C, d'Enfert C
Journal of Antimicrobial Chemotherapy - vol. 68 1285-1296 (2013)

OBJECTIVES: Candida albicans is the most prevalent fungal pathogen of humans, causing a wide range of infections from harmless superficial to severe systemic infections. Improvement of the antifungal arsenal is needed since existing antifungals can be associated with limited efficacy, toxicity and antifungal resistance. Here we aimed to identify compounds that act synergistically with echinocandin […]

Publications
Identification of a Small Molecule That Modifies MglA/SspA Interaction and Impairs Intramacrophage Survival of Francisella tularensis

PLoS ONE

Wrench AP, Gardner CL, Gonzalez CF, Lorca GL
PLoS ONE - vol. 8 1-14 (2013)

The transcription factors MglA and SspA of Francisella tularensis form a heterodimer complex and interact with the RNA polymerase to regulate the expression of the Francisella pathogenicity island (FPI) genes. These genes are essential for this pathogen’s virulence and survival within host cells. In this study, we used a small molecule screening to identify quinacrine […]

Publications
RB1 status in triple negative breast cancer cells dictates response to radiation treatment and selective therapeutic drugs

PLoS ONE

Robinson TJW, Liu JC, Vizeacoumar F, Sun T, Maclean N, Egan SE, Schimmer AD, Datti A, Zacksenhaus E
PLoS ONE - vol. 8 (2013)

Triple negative breast cancer (TNBC) includes basal-like and claudin-low subtypes for which only chemotherapy and radiation therapy are currently available. The retinoblastoma (RB1) tumor suppressor is frequently lost in human TNBC. Knockdown of RB1 in luminal BC cells was shown to affect response to endocrine, radiation and several antineoplastic drugs. However, the effect of RB1 […]

Publications
Fluorescence-Based High-Throughput Screening of Dicer Cleavage Activity

Journal of Biomolecular Screening

Podolska K, Sedlak D, Bartunek P, Svoboda P
Journal of Biomolecular Screening 1087057113497400 (2013)

Production of small RNAs by ribonuclease III Dicer is a key step in microRNA and RNA interference pathways, which employ Dicer-produced small RNAs as sequence-specific silencing guides. Further studies and manipulations of microRNA and RNA interference pathways would benefit from identification of small-molecule modulators. Here, we report a study of a fluorescence-based in vitro Dicer […]

Publications
A cell-based screening system for influenza A viral RNA transcription/replication inhibitors.

Scientific reports

Ozawa M, Shimojima M, Goto H, Watanabe S, Hatta Y, Kiso M, Furuta Y, Horimoto T, Peters NR, Hoffmann FM, Kawaoka Y
Scientific reports - vol. 3 1106 (2013)

Although two classes of antivirals, NA inhibitors and M2 ion channel blockers, are licensed for influenza treatment, dual resistant mutants, including highly pathogenic H5N1 viruses, have appeared. Alternative treatment options are, therefore, needed. Influenza A viral RNA (vRNA) transcription/replication is a promising target for antiviral development, since it is essential for virus replication. Accordingly, an […]

Publications
Dopamine D2 receptor antagonism suppresses tau aggregation and neurotoxicity

Biological Psychiatry

McCormick AV, Wheeler JM, Guthrie CR, Liachko NF, Kraemer BC
Biological Psychiatry - vol. 73 464-471 (2013)

Background: Tauopathies, including Alzheimer’s disease and frontotemporal dementia, are diseases characterized by the formation of pathological tau protein aggregates in the brain and progressive neurodegeneration. Presently no effective disease-modifying treatments exist for tauopathies. Methods: To identify drugs targeting tau neurotoxicity, we have used a Caenorhabditis elegans model of tauopathy to screen a drug library containing […]

Publications
In vitro assessment of Macleaya cordata crude extract bioactivity and anticancer properties in normal and cancerous human lung cells

Experimental and Toxicologic Pathology

Liu M, Lin YL, Chen XR, Liao CC, Poo WK
Experimental and Toxicologic Pathology - vol. 65 775-787 (2013)

The purpose of this study is to assess the bioactivity and anticancer properties of Macleaya cordata crude extract in vitro using normal fetal lung fibroblast MRC5 and adenocarcinomic epithelial cell A549 as model systems,. Treatment of extract induced cell detachment, rounding, and irregularity in shape, in both normal and adenocarcinomic human lung cells, in accompanied […]

Publications
Identification of small molecules that promote human embryonic stem cell self-renewal

Biochemical and Biophysical Research Communications

Kumagai H, Suemori H, Uesugi M, Nakatsuji N, Kawase E
Biochemical and Biophysical Research Communications - vol. 434 710-716 (2013)

Human embryonic stem cells (hESCs) and induced pluripotent cells have the potential to provide an unlimited source of tissues for regenerative medicine. For this purpose, development of defined/xeno-free culture systems under feeder-free conditions is essential for the expansion of hESCs. Most defined/xeno-free media for the culture of hESCs contain basic fibroblast growth factor (bFGF). Therefore, […]