Publications


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
A high-content image-based drug screen of clinical compounds against cell transmission of adenovirus

Nature Scientific Data

Georgi F, Kuttler F, Murer L, Andriasyan V, Witte R, Yakimovich A, Turcatti G, Greber UF
Nature Scientific Data - vol. 7 1-12 (2020)

Human adenoviruses (HAdVs) are fatal to immuno-suppressed individuals, but no effective anti-HAdV therapy is available. Here, we present a novel image-based high-throughput screening (HTS) platform, which scores the full viral replication cycle from virus entry to dissemination of progeny and second-round infections. We analysed 1,280 small molecular weight compounds of the Prestwick Chemical Library (PCL) […]

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
Bioinformatics analysis of high-throughput data to validate potential novel biomarkers and small molecule drugs for glioblastoma multiforme

Journal of International Medical Research

Qi F, Li Q, Lu X, Chen Z
Journal of International Medical Research - vol. 48 1-17 (2020)

Objective: There have been no recent improvements in the glioblastoma multiforme (GBM) outcome, with median survival remaining 15 months. Consequently, the need to identify novel biomarkers for GBM diagnosis and prognosis, and to develop targeted therapies is high. This study aimed to establish biomarkers for GBM pathogenesis and prognosis. Methods: In total, 220 overlapping differentially […]

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
Compound screening in cell-based models of tau inclusion formation: Comparison of primary neuron and HEK293 cell assays

Journal of Biological Chemistry

Crowe A, Henderson MJ, Anderson J, Titus SA, Zakharov A, Simeonov A, Buist A, Delay C, Moechars D, Trojanowski JQ, Lee VM, Brunden KR
Journal of Biological Chemistry - vol. 295 4001-4013 (2020)

The hallmark pathological features of Alzheimer’s disease (AD) brains are senile plaques, comprising β-amyloid (Aβ) peptides, and neuronal inclusions formed from tau protein. These plaques form 10 -20 years before AD symptom onset, whereas robust tau pathology is more closely associated with symptoms and correlates with cognitive status. This temporal sequence of AD pathology development, […]