Archives des Publications - Page 6 sur 44 - Prestwick Chemical Libraries

Publications

Quantitative Automated Assays in Living Cells to Screen for Inhibitors of Hemichannel Function

SLAS Discovery

Soleilhac E, Comte M, da Costa A, Barette C, Picoli C, Mortier M, Aubry L, Mouthon F, Fauvarque MO, Charvériat M
SLAS Discovery 1-8 (2020)

In vertebrates, intercellular communication is largely mediated by connexins (Cx), a family of structurally related transmembrane proteins that assemble to form hemichannels (HCs) at the plasma membrane. HCs are upregulated in different brain disorders and represent innovative therapeutic targets. Identifying modulators of Cx-based HCs is of great interest to better understand their function and define […]

Publications

High-Throughput Image-Based Aggresome Quantification

SLAS Discovery

Lesire L, Chaput L, Cruz De Casas P, Rousseau F, Piveteau C, Dumont J, Pointu D, Déprez B, Leroux F
SLAS Discovery 1-9 (2020)

Aggresomes are subcellular perinuclear structures where misfolded proteins accumulate by retrograde transport on microtubules. Different methods are available to monitor aggresome formation, but they are often laborious, time-consuming, and not quantitative. Proteostat is a red fluorescent molecular rotor dye, which becomes brightly fluorescent when it binds to protein aggregates. As this reagent was previously validated […]

Publications

Inhibition of Tryptophan Hydroxylases and Monoamine Oxidase-A by the Proton Pump Inhibitor, Omeprazole—In Vitro and In Vivo Investigations

Frontiers in Pharmacology

Betari N, Sahlholm K, Morató X, Godoy-Marín H, Jáuregui O, Teigen K, Ciruela F, Haavik J
Frontiers in Pharmacology - vol. 11 1-15 (2020)

Serotonin (5-HT) is a hormone and neurotransmitter that modulates neural activity as well as a wide range of other physiological processes including cardiovascular function, bowel motility, and platelet aggregation. 5-HT synthesis is catalyzed by tryptophan hydroxylase (TPH) which exists as two distinct isoforms; TPH1 and TPH2, which are responsible for peripheral and central 5-HT, respectively. […]

Publications

Identification of cardiac glycosides as novel inhibitors of eif4a1-mediated translation in triple-negative breast cancer cells

Cancers

Howard CM, Estrada M, Terrero D, Tiwari AK, Raman D
Cancers - vol. 12 1-18 (2020)

The eukaryotic translation initiation factor 4F complex (eIF4F) is a potential chemotherapeutic target in triple-negative breast cancer (TNBC). This complex regulates cap-dependent translational initiation and consists of three core proteins: eIF4E, eIF4G, and eIF4A1. In this study, we focus on repositioning compounds as novel inhibitors of eIF4A1-mediated translation. In order to accomplish this goal, a […]

Publications

In vitro screening of a FDA approved chemical library reveals potential inhibitors of SARS-CoV-2 replication

bioRxiv

Touret F, Gilles M, Barral K, Nougairède A, Decroly E, Lamballerie XD, Coutard B
bioRxiv 2020.04.03.023846 (2020)

A novel coronavirus, named SARS-CoV-2, emerged in 2019 from Hubei region in China and rapidly spread worldwide. As no approved therapeutics exists to treat Covid-19, the disease associated to SARS-Cov-2, there is an urgent need to propose molecules that could quickly enter into clinics. Repurposing of approved drugs is a strategy that can bypass the […]

Publications

An Unbiased Drug Screen for Seizure Suppressors in Duplication 15q Syndrome Reveals 5-HT1A and Dopamine Pathway Activation as Potential Therapies

Biological Psychiatry

Roy B, Han J, Hope KA, Peters TL, Palmer G, Reiter LT
Biological Psychiatry 1-12 (2020)

Background: Duplication 15q (Dup15q) syndrome is a rare neurogenetic disorder characterized by autism and pharmacoresistant epilepsy. Most individuals with isodicentric duplications have been on multiple medications to control seizures. We recently developed a model of Dup15q in Drosophila by elevating levels of fly Dube3a in glial cells using repo-GAL4, not neurons. In contrast to other […]

Publications

Identification of SARS-CoV-2 Inhibitors using Lung and Colonic Organoids

Nature

Han Y, Duan X, Yang L, Nilsson-Payant BE, Wang P, Duan F, Tang X, Yaron TM, Zhang T, Uhl S, Bram Y, Richardson C, Zhu J, Zhao Z, Redmond D, Houghton S, Nguyen DHT, Xu D, Wang X, Jessurun J, Borczuk A, Huang Y, Johnson JL, Liu Y, Xiang J, Wang H, Cantley LC, tenOever BR, Ho DD, Pan FC, Evans T, Chen HJ, Schwartz RE, Chen S
Nature - vol. 589 (2020)

There is an urgent need to create novel models using human disease-relevant cells to study SARS-CoV-2 biology and to facilitate drug screening. As SARS-CoV-2 primarily infects the respiratory tract, we developed a lung organoid model using human pluripotent stem cells (hPSC-LOs). The hPSC-LOs, particularly alveolar type II-like cells, are permissive to SARS-CoV-2 infection, and showed […]

Publications

Screening of potential antiviral molecules against equid herpesvirus-1 using cellular impedance measurement: Dataset of 2,891 compounds.

Data in Brief

Thieulent C, Fortier C, Munier-Lehmann H, Suzanne P, Dallemagne P, Zientara S, Hans A, Paillot R, Vidalain PO, Pronost S, Hue E
Data in Brief - vol. 33 106492 (2020)

Data presented in this article are associated with the research article “Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone and in combination” [1]. These data correspond to the in vitro screening of 2,891 potential antiviral compounds against equid herpesvirus-1 (EHV-1) based on impedance measurements using […]

Publications

HIV Drugs Inhibit Transfer of Plasmids Carrying Extended- Spectrum Beta-Lactamase and Carbapenemase Genes

mBio

Michelle M. C. Buckner A, M. Laura Ciusa ARWM, Gregory E. McCallum AELP, Alessandro Di Maio C, Piddock LJV
mBio - vol. 11 1-18 (2020)

Antimicrobial-resistant (AMR) infections pose a serious risk to human and animal health. A major factor contributing to this global crisis is the sharing of resistance genes between different bacteria via plasmids. The WHO lists Enterobacteriaceae, such as Escherichia coli and Klebsiella pneumoniae, producing extended-spectrum ␤-lactamases (ESBL) and carbapenemases as “critical” priorities for new drug development. […]

Publications

Multiple drug- induced stress responses inhibit formation of Escherichia coli biofilm

Appl Environ Microbiol

Teteneva NA MS
Appl Environ Microbiol - vol. 86 1-15 (2020)

In most ecosystems, bacteria exist primarily as structured surface-associated biofilms that can be highly tolerant to antibiotics and thus represent an important health issue. Here, we explored drug repurposing as a strategy to identify new anti- biofilm compounds, screening over 1,000 compounds from the Prestwick Chemical Library of approved drugs for specific activities that prevent […]

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