Publications

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 […]

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, […]

Journal of biomolecular screening

 Jin S, Sarkar KS, Jin YN, Liu Y, Kokel D, Van Ham TJ, Roberts LD, Gerszten RE, Macrae CA, Peterson RT
 Journal of biomolecular screening - vol. 18 108-115 (2013)

Organophosphates are a class of highly toxic chemicals that includes many pesticides and chemical weapons. Exposure to organophosphates, either through accidents or acts of terrorism, poses a significant risk to human health and safety. Existing antidotes, in use for over 50 years, have modest efficacy and undesirable toxicities. Therefore, discovering new organophosphate antidotes is a […]

Drug Discovery Today: Technologies

 Kawahara G, Kunkel LM
 Drug Discovery Today: Technologies - vol. 10 e91-e96 (2013)

Recently, a number of chemical and drug screens using zebrafish embryos have been published. Using zebrafish dystrophin mutants, we screened a chemical library for small molecules that modulate the muscle phenotype and identified seven small molecules that influence muscle pathology in dystrophin-null zebrafish. One chemical, aminophylline, which is known to be a non-selective phosphodiesterase (PDE) […]

Bioorganic and Medicinal Chemistry

 Gozalbes R, Mosulén S, Ortí L, Rodríguez-Díaz J, Carbajo RJ, Melnyk P, Pineda-Lucena A
 Bioorganic and Medicinal Chemistry - vol. 21 1944-1951 (2013)

Heparanase is a key enzyme involved in the dissemination of metastatic cancer cells. In this study a combination of in silico techniques and experimental methods was used to identify new potential inhibitors against this target. A 3D model of heparanase was built from sequence homology and applied to the virtual screening of a library composed […]

Applied Microbiology and Biotechnology

 Antoniani D, Rossi E, Rinaldo S, Bocci P, Lolicato M, Paiardini A, Raffaelli N, Cutruzzol?? F, Landini P
 Applied Microbiology and Biotechnology - vol. 97 7325-7336 (2013)

In Gram-negative bacteria, production of the signal molecule c-di-GMP by diguanylate cyclases (DGCs) is a key trigger for biofilm formation, which, in turn, is often required for the development of chronic bacterial infections. Thus, DGCs represent interesting targets for new chemotherapeutic drugs with anti-biofilm activity. We searched for inhibitors of the WspR protein, a Pseudomonas […]

Drug Discovery Today: Technologies

 Chartier A, Simonelig M
 Drug Discovery Today: Technologies - vol. 10 e103-e108 (2013)

Oculopharyngeal muscular dystrophy (OPMD) is a late onset disease which affects specific muscles. No pharmacological treatments are currently available for OPMD. In recent years, genetically tractable models of OPMD-Drosophila and Caenorhabditis elegans-have been generated. Although these models have not yet been used for large-scale primary drug screening, they have been very useful in candidate approaches […]

PLoS ONE

 Dahlin JL, Sinville R, Solberg J, Zhou H, Han J, Francis S, Strasser JM, John K, Hook DJ, Walters MA, Zhang Z
 PLoS ONE - vol. 8 (2013)

The lysine acetyltransferase (KAT) Rtt109 forms a complex with Vps75 and catalyzes the acetylation of histone H3 lysine 56 (H3K56ac) in the Asf1-H3-H4 complex. Rtt109 and H3K56ac are vital for replication-coupled nucleosome assembly and genotoxic resistance in yeast and pathogenic fungal species such as Candida albicans. Remarkably, sequence homologs of Rtt109 are absent in humans. […]

Journal of biomolecular screening

 Bharat A, Blanchard JE, Brown ED
 Journal of biomolecular screening - vol. 18 830-836 (2013)

The synthesis of ribosomes is an essential process, which is aided by a variety of trans-acting factors in bacteria. Among these is a group of GTPases essential for bacterial viability and emerging as promising targets for new antibacterial agents. Herein, we describe a robust high-throughput screening process for inhibitors of one such GTPase, the Escherichia […]

Biochimica et Biophysica Acta - Molecular Cell Research

 Audran E, Dagher R, Gioria S, Tsvetkov PO, Kulikova AA, Didier B, Villa P, Makarov AA, Kilhoffer MC, Haiech J
 Biochimica et Biophysica Acta - Molecular Cell Research - vol. 1833 1720-1731 (2013)

The prominent role of Ca2+ in cell physiology is mediated by a whole set of proteins involved in Ca2+-signal generation, deciphering and arrest. Among these intracellular proteins, calmodulin (CaM) known as a prototypical calcium sensor, serves as a ubiquitous carrier of the intracellular calcium signal in all eukaryotic cell types. CaM is assumed to be […]

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