Archives des Publications - Page 15 sur 44 - Prestwick Chemical Libraries

Publications


Publications
Development of a Cell-Based Fluorescence Polarization Biosensor Using Preproinsulin to Identify Compounds That Alter Insulin Granule Dynamics.

Assay and drug development technologies

Yi NY, He Q, Caligan TB, Smith GR, Forsberg LJ, Brenman JE, Sexton JZ
Assay and drug development technologies - vol. 13 558-569 (2015)

Diabetes currently affects 9.3% of the U.S. population totaling $245 billion annually in U.S. direct and indirect healthcare costs. Current therapies for diabetes are limited in their ability to control blood glucose and/or enhance insulin sensitivity. Therefore, innovative and efficacious therapies for diabetes are urgently needed. Herein we describe a fluorescent insulin reporter system (preproinsulin-mCherry, […]

Publications
Novel activities of select NSAID renantiomers against Rac1 and Cdc42 GTPases

PLoS ONE

Oprea TI, Sklar LA, Agola JO, Guo Y, Silberberg M, Roxby J, Vestling A, Romero E, Surviladze Z, Murray-Krezan C, Waller A, Ursu O, Hudson LG, Wandinger-Ness A
PLoS ONE - vol. 10 1-32 (2015)

Rho family GTPases (including Rac, Rho and Cdc42) collectively control cell proliferation, adhesion and migration and are of interest as functional therapeutic targets in numerous epithelial cancers. Based on high throughput screening of the Prestwick Chemical Library® and cheminformatics we identified the R-enantiomers of two approved drugs (naproxen and ketorolac) as inhibitors of Rac1 and […]

Publications
A chemical screen to identify inducers of the mitochondrial unfolded protein response in C. elegans

Worm

Rauthan M, Pilon M
Worm - vol. 4 e1096490 (2015)

Publications
Clobetasol and halcinonide act as smoothened agonists to promote myelin gene expression and RxRγ receptor activation

PLoS ONE

Porcu G, Serone E, De Nardis V, Di Giandomenico D, Lucisano G, Scardapane M, Poma A, Ragnini-Wilson A
PLoS ONE - vol. 10 1-22 (2015)

One of the causes of permanent disability in chronic multiple sclerosis patients is the inability of oligodendrocyte progenitor cells (OPCs) to terminate their maturation program at lesions. To identify key regulators of myelin gene expression acting at the last stages of OPC maturation we developed a drug repositioning strategy based on the mouse immortalized oligodendrocyte […]

Publications
Yeast as a system for modeling mitochondrial disease mechanisms and discovering therapies

Disease Models & Mechanisms

Lasserre J, Dautant A, Aiyar RS, Kucharczyk R, Glatigny A, Tribouillard-Tanvier D, Rytka J, Blondel M, Skoczen N, Reynier P, Pitayu L, Rotig A, Delahodde A, Steinmetz LM, Dujardin G, Procaccio V, di Rago J
Disease Models & Mechanisms - vol. 8 509-526 (2015)

Mitochondrial diseases are severe and largely untreatable. Owing to the many essential processes carried out by mitochondria and the complex cellular systems that support these processes, these diseases are diverse, pleiotropic, and challenging to study. Much of our current understanding of mitochondrial function and dysfunction comes from studies in the baker’s yeast Saccharomyces cerevisiae. Because […]

Publications
A role for fragment-based drug design in developing novel lead compounds for central nervous system targets

Frontiers in Neurology

Wasko MJ, Pellegrene KA, Madura JD, Surratt CK
Frontiers in Neurology - vol. 6 1-11 (2015)

Hundreds of millions of U.S. dollars are invested in the research and development of a single drug. Lead compound development is an area ripe for new design strategies. Therapeutic lead candidates have been traditionally found using high-throughput in vitro pharmacological screening, a costly method for assaying thousands of compounds. This approach has recently been augmented […]

Publications
Efficient Generation of Cardiac Purkinje Cells from ESCs by Activating cAMP Signaling

Stem Cell Reports

Tsai SY, Maass K, Lu J, Fishman GI, Chen S, Evans T
Stem Cell Reports - vol. 4 1089-1102 (2015)

Dysfunction of the specialized cardiac conduction system (CCS) is associated with life-threatening arrhythmias. Strategies to derive CCS cells, including rare Purkinje cells (PCs), would facilitate models for mechanistic studies and drug discovery and also provide new cellular materials for regenerative therapies. A high-throughput chemical screen using CCS:lacz and Contactin2:egfp (Cntn2:egfp) reporter embryonic stem cell (ESC) […]

Publications
A Multiplexed Cell-Based Assay for the Identification of Modulators of Pre-Membrane Processing as a Target against Dengue Virus.

Journal of biomolecular screening

Stolp ZD, Smurthwaite CA, Reed C, Williams W, Dharmawan A, Djaballah H, Wolkowicz R
Journal of biomolecular screening - vol. 20 616-26 (2015)

The DenV pre-membrane protein (prM) is a crucial chaperone for the viral envelope protein, preventing premature fusion with vesicles during viral export. prM molecules in immature particles are cleaved by host proteases, leading to mature fusogenic virions. Blockade of prM cleavage would restrict fusion and represents a novel druggable opportunity against DenV. We have thus […]

Publications
Apoptosis induced by NAD depletion is inhibited by KN-93 in a CaMKII-independent manner.

Experimental cell research

Takeuchi M, Yamamoto T
Experimental cell research - vol. 335 62-67 (2015)

Nicotinamide phosphoribosyltransferase (NAMPT) is a key enzyme that catalyzes the synthesis of nicotinamide mononucleotide from nicotinamide (Nam) in the salvage pathway of mammalian NAD biosynthesis. Several potent NAMPT inhibitors have been identified and used to investigate the role of intracellular NAD and to develop therapeutics. NAD depletion induced by NAMPT inhibitors depolarizes mitochondrial membrane potential […]

Publications
Lansoprazole is an antituberculous prodrug targeting cytochrome bc1.

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 […]