Archives des Publications - Page 8 sur 46 - Prestwick Chemical Libraries

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 […]

Publications

Chlorambucil targets BRCA 1/2‐deficient tumours and counteracts PARP inhibitor resistance

EMBO Molecular Medicine

Tacconi EM, Badie S, De Gregoriis G, Reisländer T, Lai X, Porru M, Folio C, Moore J, Kopp A, Baguña Torres J, Sneddon D, Green M, Dedic S, Lee JW, Batra AS, Rueda OM, Bruna A, Leonetti C, Caldas C, Cornelissen B, Brino L, Ryan A, Biroccio A, Tarsounas M
EMBO Molecular Medicine - vol. 11 1-16 (2019)

© 2019 The Authors. Published under the terms of the CC BY 4.0 license Due to compromised homologous recombination (HR) repair, BRCA1- and BRCA2-mutated tumours accumulate DNA damage and genomic rearrangements conducive of tumour progression. To identify drugs that target specifically BRCA2-deficient cells, we screened a chemical library containing compounds in clinical use. The top […]

Publications

Repurposing of ribavirin as an adjunct therapy against invasive Candida strains in an in vitro study

Antimicrobial Agents and Chemotherapy

Yousfi H, Cassagne C, Ranque S, Rolain JM, Bittar F
Antimicrobial Agents and Chemotherapy - vol. 63 1-8 (2019)

The use of antifungal agents in clinical settings is limited by the appearance of drug resistance and adverse side effects. There is, therefore, an urgent need to develop new drugs to strengthen the treatment of invasive fungal diseases. The aim of this study is to describe the potential repurposing of ribavirin as an adjunct therapy […]

Publications

Novel drug candidates for treating esophageal carcinoma: A study on differentially expressed genes, using connectivity mapping and molecular docking

International Journal of Oncology

Chen YT, Xie JY, Sun Q, Mo WJ
International Journal of Oncology - vol. 54 152-166 (2019)

Patients with esophageal carcinoma (ESCA) have a poor prognosis and high mortality rate. Although standard therapies have had effect, there is an urgent requirement to develop novel options, as increasing drug tolerance has been identifiedinclinicalpractice.Inthepresentstudy,differentially expressedgenes(DEGs)ofESCAwereidentifiedinTheCancer Genome Atlas and Genotype-Tissue Expression databases. Functional and protein-protein interaction (PPI) analyses were performed. The Connectivity Map (CMAP) was […]

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