Archives des Publications - Page 24 sur 46 - Prestwick Chemical Libraries

Publications

Development of a high-throughput screening cancer cell-based luciferase refolding assay for identifying Hsp90 inhibitors.

Assay and drug development technologies

Sadikot T, Swink M, Eskew JD, Brown D, Zhao H, Kusuma BR, Rajewski RA, Blagg BSJ, Matts RL, Holzbeierlein JM, Vielhauer GA
Assay and drug development technologies - vol. 11 478-488 (2013)

The 90 kDa heat-shock protein (Hsp90) and other cochaperones allow for proper folding of nascent or misfolded polypeptides. Cancer cells exploit these chaperones by maintaining the stability of mutated and misfolded oncoproteins and allowing them to evade proteosomal degradation. Inhibiting Hsp90 is an attractive strategy for cancer therapy, as the concomitant degradation of multiple oncoproteins […]

Publications

High-throughput screening of a collection of known pharmacologically active small compounds for identification of candida albicans biofilm inhibitors

Antimicrobial Agents and Chemotherapy

Siles SA, Srinivasan A, Pierce CG, Lopez-Ribot JL, Ramasubramanian AK
Antimicrobial Agents and Chemotherapy - vol. 57 3681-3687 (2013)

Candida albicans is the most common etiologic agent of systemic fungal infections with unacceptably high mortality rates. The existing arsenal of antifungal drugs is very limited and is particularly ineffective against C. albicans biofilms. To address the unmet need for novel antifungals, particularly those active against biofilms, we have screened a small molecule library consisting […]

Publications

Metformin impairs glucose consumption and survival in Calu-1 cells by direct inhibition of hexokinase-II.

Scientific reports

Salani B, Marini C, Rio AD, Ravera S, Massollo M, Orengo AM, Amaro A, Passalacqua M, Maffioli S, Pfeffer U, Cordera R, Maggi D, Sambuceti G
Scientific reports - vol. 3 1-8 (2013)

The anti-hyperglycaemic drug metformin has important anticancer properties as shown by the direct inhibition of cancer cells proliferation. Tumor cells avidly use glucose as a source for energy production and cell building blocks. Critical to this phenotype is the production of glucose-6-phosphate (G6P), catalysed by hexokinases (HK) I and II, whose role in glucose retention […]

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 […]

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