Publications

Nature communications

 Rybniker J, Vocat A, Sala C, Busso P, Pojer F, Benjak A, Cole ST
 Nature communications - vol. 6 1-8 (2015)

Better antibiotics capable of killing multi-drug-resistant Mycobacterium tuberculosis are urgently needed. Despite extensive drug discovery efforts, only a few promising candidates are on the horizon and alternative screening protocols are required. Here, by testing a panel of FDA-approved drugs in a host cell-based assay, we show that the blockbuster drug lansoprazole (Prevacid), a gastric proton-pump […]

Brain

 Teixeira-Castro A, Jalles A, Esteves S, Kang S, Da Silva Santos L, Silva-Fernandes A, Neto MF, Brielmann RM, Bessa C, Duarte-Silva S, Miranda A, Oliveira S, Neves-Carvalho A, Bessa J, Summavielle T, Silverman RB, Oliveira P, Morimoto RI, Maciel P
 Brain - vol. 138 3221-3237 (2015)

Polyglutamine diseases are a class of dominantly inherited neurodegenerative disorders for which there is no effective treatment. Here we provide evidence that activation of serotonergic signalling is beneficial in animal models of Machado-Joseph disease. We identified citalopram, a selective serotonin reuptake inhibitor, in a small molecule screen of FDA-approved drugs that rescued neuronal dysfunction and […]

Molecular Oncology

 Srivastava G, Matta A, Fu G, Somasundaram RT, Datti A, Walfish PG, Ralhan R
 Molecular Oncology - vol. 9 1720-1735 (2015)

Oral squamous cell carcinoma (OSCC) patients diagnosed in late stages have limited chemotherapeutic options, underscoring the great need for development of new anticancer agents for more effective disease management. We aimed to identify novel anticancer agents for OSCC using quantitative high throughput assays for screening six chemical libraries consisting of 5170 small molecule inhibitors. In […]

Breast cancer research

 Ren X, Wang J, Osada T, Mook RA, Morse MA, Barak LS, Lyerly HK, Chen W
 Breast cancer research - vol. 17 1-11 (2015)

INTRODUCTION: Human epidermal growth factor receptor HER3 has been implicated in promoting the aggressiveness and metastatic potential of breast cancer. Upregulation of HER3 has been found to be a major mechanism underlying drug resistance to EGFR and HER2 tyrosine kinase inhibitors and to endocrine therapy in the treatment of breast cancer. Thus, agents that reduce […]

Journal of Biomolecular Screening

 Malergue F, van Agthoven A, Scifo C, Egan D, Strous GJ
 Journal of Biomolecular Screening - vol. 20 416-421 (2015)

Drug discovery often requires the screening of compound libraries on tissue cultured cells. Some major targets in drug discovery belong to signal transduction pathways, and PerFix EXPOSE* allows easy flow cytometry phospho assays. We thus investigated the possibility to further simplify and automate this assay, to allow the direct screening of drugs targeting signaling pathways. […]

Toxicology Letters

 Ratajewski M, Grzelak I, Wi??niewska K, Ryba K, Gorzkiewicz M, Walczak-Drzewiecka A, Hoffmann M, Dastych J
 Toxicology Letters - vol. 232 193-202 (2015)

The pregnane X receptor (PXR) is one of the master regulators of xenobiotic transformation. Interactions between pharmacologic compounds and PXR frequently result in drug-to-drug interactions, drug-induced hepatotoxicity, and the development of drug-resistant phenotypes in cancer cells. Potential PXR-mediated effects on drug metabolism can be predicted using high-throughput methods to detect PXR transactivation. We used the […]

Integrative biology : quantitative biosciences from nano to macro

 Park CY, Zhou EH, Tambe D, Chen B, Lavoie T, Dowell M, Simeonov A, Maloney DJ, Marinkovic A, Tschumperlin DJ, Burger S, Frykenberg M, Butler JP, Stamer WD, Johnson M, Solway J, Fredberg JJ, Krishnan R
 Integrative biology : quantitative biosciences from nano to macro - vol. 7 1-16 (2015)

When cellular contractile forces are central to pathophysiology, these forces comprise a logical target of therapy. Nevertheless, existing high-throughput screens are limited to upstream signalling intermediates with poorly defined relationships to such a physiological endpoint. Using cellular force as the target, here we report a new screening technology and demonstrate its applications using human airway […]

Journal of biomolecular screening

 Pedram Fatemi R, Salah-Uddin S, Modarresi F, Khoury N, Wahlestedt C, Faghihi MA
 Journal of biomolecular screening - vol. 20 1132-41 (2015)

Long non-protein coding RNAs (lncRNAs) are an important class of molecules that help orchestrate key cellular events. Although their functional roles in cells are not well understood, thousands of lncRNAs and a number of possible mechanisms by which they act have been reported. LncRNAs can exert their regulatory function in cells by interacting with epigenetic […]

Journal of biomolecular screening

 Raneri M, Sciandrone B, Briani F
 Journal of biomolecular screening - vol. 20 627-33 (2015)

The bacterial translational apparatus is an ideal target for the search of new antibiotics. In fact, it performs an essential process carried out by a large number of potential subtargets for antibiotic action. Moreover, it is sufficiently different in several molecular details from the apparatus of Eukarya and Archaea to generally ensure specificity for the […]

Trends in Pharmacological Sciences

 Keillor JW, Apperley KYP, Akbar A
 Trends in Pharmacological Sciences - vol. 36 32-40 (2015)

Tissue transglutaminase (TG2) catalyzes the cross-linking of proteins by the formation of isopeptide bonds between glutamine (Gln) and lysine (Lys) side chains. Although TG2 is essential for the stabilization of the extracellular matrix, its unregulated activity has been implicated in celiac disease, fibrosis, and cancer metastasis, among other disorders. Given the importance and range of […]

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