Theorell J, Gustavsson AL, Tesi B, Sigmundsson K, Ljunggren HG, Lundbäck T, Bryceson YT
Cancer Immunology, Immunotherapy - vol. 63 627-641 (2014)
Filgueira CS, Benod C, Lou X, Gunamalai PS, Villagomez RA, Strom A, Gustafsson J, Berkenstam AL, Webb P
Nuclear Receptor Signaling - vol. 12 1-13 (2014)
The establishment of effective high throughput screening cascades to identify nuclear receptor (NR) ligands that will trigger defined, therapeutically useful sets of NR activities is of considerable importance. Repositioning of existing approved drugs with known side effect profiles can provide advantages because de novo drug design suffers from high developmental failure rates and undesirable side […]
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 […]
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 […]
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 […]
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 […]
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. […]
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 […]
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 […]
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 […]
