Archives des Publications - Page 17 sur 44 - Prestwick Chemical Libraries

Publications

Fluorescence polarization screening assays for small molecule allosteric modulators of ABL kinase function

PLoS ONE

Grover P, Shi H, Baumgartner M, Camacho CJ, Smithgall TE
PLoS ONE - vol. 10 1-26 (2015)

The ABL protein-tyrosine kinase regulates intracellular signaling pathways controlling diverse cellular processes and contributes to several forms of cancer. The kinase activity of ABL is repressed by intramolecular interactions involving its regulatory Ncap, SH3 and SH2 domains. Small molecules that allosterically regulate ABL kinase activity through its non-catalytic domains may represent selective probes of ABL […]

Publications

Applications of flow cytometry for measurement of autophagy

Methods

Demishtein A, Porat Z, Elazar Z, Shvets E
Methods - vol. 75 87-95 (2015)

Autophagy is a dynamic catabolic process that plays a major role in sequestering and recycling cellular components in multiple physiological and pathophysiological conditions. Despite recent progress in our understanding of the autophagic process there is still a shortage of robust methods for monitoring autophagy in live cells. Flow cytometry, a reliable and unbiased method for […]

Publications

G protein-coupled receptor 35: An emerging target in inflammatory and cardiovascular disease

Frontiers in Pharmacology

Divorty N, Mackenzie AE, Nicklin SA, Milligan G
Frontiers in Pharmacology - vol. 6 1-13 (2015)

G protein-coupled receptor 35 (GPR35) is an orphan receptor, discovered in 1998, that has garnered interest as a potential therapeutic target through its association with a range of diseases. However, a lack of pharmacological tools and the absence of convincingly defined endogenous ligands have hampered the understanding of function necessary to exploit it therapeutically. Although […]

Publications

Preclinical combination therapy of the investigational drug NAMI-A⁺ with doxorubicin for mammary cancer

Investigational New Drugs

Bergamo A, Riedel T, Dyson PJ, Sava G
Investigational New Drugs - vol. 33 53-63 (2015)

AIM OF THE STUDY: The tumor metastases targeting ruthenium complex NAMI-A synergistically improves the activity of gemcitabine in combination therapies. High-throughput screening was used to identify other potential drug combinations from a library of FDA approved drugs. Doxorubicin was identified as a hit compound and was therefore evaluated in combination with NAMI-A in vitro and […]

Publications

Identification of new MRP4 inhibitors from a library of FDA approved drugs using a high-throughput bioluminescence screen

Biochemical Pharmacology

Cheung L, Yu DMT, Neiron Z, Failes TW, Arndt GM, Fletcher JI
Biochemical Pharmacology - vol. 93 380-388 (2015)

Multidrug resistance protein 4 (MRP4) effluxes a wide variety of drugs and endogenous signaling molecules from cells and has been proposed as an attractive therapeutic target in several solid tumors, including neuroblastoma and colorectal cancer. MRP4 also regulates the pharmacokinetics of its drug substrates and its absence can increase their tissue penetration. We observed that […]

Publications

Identification of Nitazoxanide as a Group I Metabotropic Glutamate Receptor Negative Modulator for the Treatment of Neuropathic Pain: An In Silico Drug Repositioning Study.

Pharmaceutical research

Ai N, Wood RD, Welsh WJ
Pharmaceutical research - vol. 32 2798-807 (2015)

PURPOSE: Drug repositioning strategies were employed to explore new therapeutic indications for existing drugs that may exhibit dual negative mGluR1/5 modulating activities as potential treatments for neuropathic pain. METHOD: A customized in silico-in vitro-in vivo drug repositioning scheme was assembled and implemented to search available drug libraries for compounds with dual mGluR1/5 antagonistic activities, that […]

Publications

Identification of quorum-sensing inhibitors disrupting signaling between rgg and short hydrophobic peptides in streptococci

mBio

Aggarwal C, Jimenez JC, Lee H, Chlipala GE, Ratia K, Federle MJ
mBio - vol. 6 1-11 (2015)

Bacteria coordinate a variety of social behaviors, important for both environmental and pathogenic bacteria, through a process of intercellular chemical signaling known as quorum sensing (QS). As microbial resistance to antibiotics grows more common, a critical need has emerged to develop novel anti-infective therapies, such as an ability to attenuate bacterial pathogens by means of […]

Publications

Tamoxifen inhibits CDK5 kinase activity by interacting with p35/p25 and modulates the pattern of tau phosphorylation

Chemistry and Biology

Corbel C, Zhang B, Le Parc A, Baratte B, Colas P, Couturier C, Kosik KS, Landrieu I, Le Tilly V, Bach S
Chemistry and Biology - vol. 22 472-482 (2015)

Cyclin-dependent kinase 5 (CDK5) is a multifunctional enzyme that plays numerous roles, notably in brain development. CDK5 is activated through its association with the activators, p35 and p39, rather than by cyclins. Proteolytic procession of the N-terminal part of its activators has been linked to Alzheimer’s disease and various other neuropathies. The interaction with the […]

Publications

PTPMT1 inhibition lowers glucose through succinate dehydrogenase phosphorylation

Cell Reports

Nath AK, Ryu JH, Jin YN, Roberts LD, Dejam A, Gerszten RE, Peterson RT
Cell Reports - vol. 10 694-701 (2015)

Virtually all organisms seek to maximize fitness by matching fuel availability with energy expenditure. In vertebrates, glucose homeostasis is central to this process, with glucose levels finely tuned to match changing energy requirements. To discover new pathways regulating glucose levels invivo, we performed a large-scale chemical screen in live zebrafish and identified the small molecule […]

Publications

Development of A Cell-Based Assay to Identify Small Molecule Inhibitors of FGF23 Signaling

ASSAY and Drug Development Technologies

Diener S, Schorpp K, Strom T, Hadian K, Lorenz-Depiereux B
ASSAY and Drug Development Technologies - vol. 13 476-487 (2015)

Abstract Fibroblast growth factor 23 (FGF23) is a bone-derived endocrine key regulator of phosphate homeostasis. It inhibits renal tubular phosphate reabsorption by activating receptor complexes composed of FGF receptor 1c (FGFR1c) and the co-receptor Klotho. As a major signaling pathway mitogen-activated protein kinase (MAPK) pathway is employed. In this study, we established an FGF23-inducible cell […]

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