Archives des Publications - Page 20 sur 44 - Prestwick Chemical Libraries

Publications


Publications
Induction of covalently crosslinked p62 oligomers with reduced binding to polyubiquitinated proteins by the autophagy inhibitor verteporfin

PLoS ONE

Donohue E, Balgi AD, Komatsu M, Roberge M
PLoS ONE - vol. 9 1-30 (2014)

Autophagy is a cellular catabolic process responsible for the degradation of cytoplasmic constituents, including organelles and long-lived proteins, that helps maintain cellular homeostasis and protect against various cellular stresses. Verteporfin is a benzoporphyrin derivative used clinically in photodynamic therapy to treat macular degeneration. Verteporfin was recently found to inhibit autophagosome formation by an unknown mechanism […]

Publications
Energetics-based methods for protein folding and stability measurements.

Annual review of analytical chemistry (Palo Alto, Calif.)

Geer MA, Fitzgerald MC
Annual review of analytical chemistry (Palo Alto, Calif.) - vol. 7 209-28 (2014)

Over the past 15 years, a series of energetics-based techniques have been developed for the thermodynamic analysis of protein folding and stability. These techniques include Stability of Unpurified Proteins from Rates of amide H/D Exchange (SUPREX), pulse proteolysis, Stability of Proteins from Rates of Oxidation (SPROX), slow histidine H/D exchange, lysine amidination, and quantitative cysteine […]

Publications
Expanding the scope of drug repurposing in pediatrics: The Children’s Pharmacy Collaborative???

Drug Discovery Today

Blatt J, Farag S, Corey SJ, Sarrimanolis Z, Muratov E, Fourches D, Tropsha A, Janzen WP
Drug Discovery Today - vol. 19 1696-1698 (2014)

Drug repurposing is the use of ‘old’ drugs for new indications, avoiding the need for time- and cost-intensive toxicity studies. This approach should be particularly attractive for pediatrics, but its use in this population has been limited. One obstacle has been the lack of a comprehensive database of drugs for which there already is at […]

Publications
Chalcones as positive allosteric modulators of ??7 nicotinic acetylcholine receptors: A new target for a privileged structure

European Journal of Medicinal Chemistry

Balsera B, Mulet J, Fernández-Carvajal A, Torre-Martínez RDL, Ferrer-Montiel A, Hernández-Jiménez JG, Estévez-Herrera J, Borges R, Freitas AE, López MG, García-López MT, González-Muñiz R, Pérez De Vega MJ, Valor LM, Svobodová L, Sala S, Sala F, Criado M
European Journal of Medicinal Chemistry - vol. 86 724-739 (2014)

The alpha-7 acetylcholine nicotine receptor is a ligand-gated ion channel that is involved in cognition disorders, schizophrenia, pain and inflammation among other diseases. Therefore, the development of new agents that target this receptor has great significance. Positive allosteric modulators might be advantageous, since they facilitate receptor responses without directly interacting with the agonist binding site. […]

Publications
5-azacytidine inhibits nonsense-mediated decay in a MYC-dependent fashion

EMBO molecular medicine

Bhuvanagiri M, Lewis J, Putzker K, Becker JP, Leicht S, Krijgsveld J, Batra R, Turnwald B, Jovanovic B, Hauer C, Sieber J, Hentze MW, Kulozik AE
EMBO molecular medicine - vol. 6 1593-1609 (2014)

Nonsense-mediated RNA decay (NMD) is an RNA-based quality control mechanism that eliminates transcripts bearing premature translation termination codons (PTC). Approximately, one-third of all inherited disorders and some forms of cancer are caused by nonsense or frame shift mutations that introduce PTCs, and NMD can modulate the clinical phenotype of these diseases. 5-azacytidine is an analogue […]

Publications
A Basic Post-SET Extension of NSDs Is Essential for Nucleosome Binding In Vitro.

Journal of biomolecular screening

Allali-Hassani A, Kuznetsova E, Hajian T, Wu H, Dombrovski L, Li Y, Gräslund S, Arrowsmith CH, Schapira M, Vedadi M
Journal of biomolecular screening - vol. 19 928-935 (2014)

The nuclear receptor SET domain-containing family of proteins (NSD1, NSD2, and NSD3) is known to mono- and dimethylate lysine 36 of histone H3 (H3K36). Overexpression and translocation of NSDs have been widely implicated in a variety of diseases including cancers. Although the substrate specificity of NSDs has been a subject of many valuable studies, the […]

Publications
Cytochrome P450 2C epoxygenases mediate photochemical stress-induced death of photoreceptors

Journal of Biological Chemistry

Chang Q, Berdyshev E, Cao D, Bogaard JD, White JJ, Chen S, Shah R, Mu W, Grantner R, Bettis S, Grassi MA
Journal of Biological Chemistry - vol. 289 8337-8352 (2014)

Degenerative loss of photoreceptors occurs in inherited and age-related retinal degenerative diseases. Chemical screen facilitates development of new testing routes for neuroprotection and mechanistic investigation. Herein, we conducted a mouse-derived photoreceptor (661W cells)-based high throughput screen of the FDA-approved Prestwick drug library to identify putative cytoprotective compounds against light-induced, synthetic visual chromophore-precipitated cell death. Different […]

Publications
Drug-repositioning screening identified piperlongumine as a direct STAT3 inhibitor with potent activity against breast cancer.

Oncogene

Bharadwaj U, Eckols TK, Kolosov M, Kasembeli MM, Adam A, Torres D, Zhang X, Dobrolecki LE, Wei W, Lewis MT, Dave B, Chang JC, Landis MD, Creighton CJ, Mancini MA, Tweardy DJ
Oncogene 1-13 (2014)

Signal transducer and activator of transcription (STAT) 3 regulates many cardinal features of cancer including cancer cell growth, apoptosis resistance, DNA damage response, metastasis, immune escape, tumor angiogenesis, the Warburg effect and oncogene addiction and has been validated as a drug target for cancer therapy. Several strategies have been used to identify agents that target Stat3 in […]

Publications
An automated high-throughput cell-based multiplexed flow cytometry assay to identify novel compounds to target Candida albicansvirulence-related proteins

PLoS ONE

Bernardo SM, Allen CP, Waller A, Young SM, Oprea T, Sklar LA, Lee SA
PLoS ONE - vol. 9 1-11 (2014)

Although three major classes of systemic antifungal agents are clinically available, each is characterized by important limitations. Thus, there has been considerable ongoing effort to develop novel and repurposed agents for the therapy of invasive fungal infections. In an effort to address these needs, we developed a novel high-throughput, multiplexed screening method that utilizes small […]

Publications
Repositioning drugs for inflammatory disease-fishing for new anti-inflammatory agents.

Disease models & mechanisms

Hall CJ, Wicker SM, Chien A, Tromp A, Lawrence LM, Sun X, Krissansen GW, Crosier KE, Crosier PS
Disease models & mechanisms - vol. 7 1069-1081 (2014)

Inflammation is an important and appropriate host response to infection or injury. However, dysregulation of this response, with resulting persistent or inappropriate inflammation, underlies a broad range of pathological processes, from inflammatory dermatoses to type 2 diabetes and cancer. As such, identifying new drugs to suppress inflammation is an area of intense interest. Despite notable […]