Publications (2018-2020)

Publications (2018-2020) Identification of cardiac glycosides as novel inhibitors of eif4a1-mediated translation in triple-negative breast cancer cells.

Howard, C. M., Estrada, M., Terrero, D., Tiwari, A. K. & Raman, D.
Cancers (Basel) 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 (2018-2020) The first wide-scale drug repurposing screen using the Prestwick Chemical Library (1200 bioactive molecules) against Neisseria gonorrhoeae identifies high in vitro activity of auranofin and many additional drugs.

Foerster, S. et al.
Apmis 128 242–250 (2020)

Treatment options for gonorrhoea are scarce. Drug repurposing of bioactive molecules approved for other conditions might therefore be of value. We developed a method for wide-scale, systematic drug repurposing screen to identify molecules with activity against Neisseria gonorrhoeae and screened the Prestwick Chemical Library (1200 FDA-approved drugs). As a proof-of-concept, we further examined one promising […]

Publications (2018-2020) Identification of repositionable drugs with novel antimycotic activity by screening the Prestwick Chemical Library against emerging invasive moulds.

Yousfi, H., Ranque, S., Cassagne, C., Rolain, J. M. & Bittar, F.
J. Glob. Antimicrob. Resist. 21 314–317 (2020)

Objectives: The incidence of severe filamentous fungal infections has increased over the past decade. Some of these filamentous fungi are resistant to available antifungals; it is thus urgent to find new compounds that are active against such life-threatening pathogens. Methods: In this study, 1280 drugs (Prestwick Chemical Library) were tested against six multidrug-resistant (MDR) filamentous fungi, includingAspergillus, […]

Publications (2018-2020) High content drug screening for Fanconi anemia therapeutics.

Montanuy, H. et al.
Orphanet J. Rare Dis. 15 1–9 (2020)

Background Fanconi anemia is a rare disease clinically characterized by malformations, bone marrow failure and an increased risk of solid tumors and hematologic malignancies. The only therapies available are hematopoietic stem cell transplantation for bone marrow failure or leukemia, and surgical resection for solid tumors. Therefore, there is still an urgent need for new therapeutic […]

Publications (2018-2020) Drosophila SMN2 minigene reporter model identifies moxifloxacin as a candidate therapy for SMA

Konieczny, P. & Artero, R.
FASEB J. 34 3021–3036 (2020)

Spinal muscular atrophy is a rare and fatal neuromuscular disorder caused by the loss of alpha motor neurons. The affected individuals have mutated the ubiquitously expressed SMN1 gene resulting in the loss or reduction in the survival motor neuron (SMN) protein levels. However, an almost identical paralog exists in humans: SMN2. Pharmacological activation of SMN2 […]

Publications (2018-2020) Quantitative Automated Assays in Living Cells to Screen for Inhibitors of Hemichannel

Soleilhac, E. et al.
Function. SLAS Discov. (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 (2018-2020) High-Throughput Image-Based Aggresome Quantification.

Lesire, L. et al.
SLAS Discov. 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 (2018-2020) In vitro screening of a FDA approved chemical library reveals potential inhibitors of SARS-CoV-2 replication.

Touret, F. et al.
Scientific Reports View all Nature Research journals Search Login (2020)

A novel coronavirus, named SARS-CoV-2, emerged in 2019 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 time-consuming stages of […]

Publications (2018-2020) An Unbiased Drug Screen for Seizure Suppressors in Duplication 15q Syndrome Reveals 5-HT1A and Dopamine Pathway Activation as Potential Therapies.

Roy, B. et al.
Biol. 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 Dup15q models, these flies develop […]

Publications (2018-2020) New multidrug efflux inhibitors for gram-negative bacteria

Marshall, R. L. et al.
MBio 11 1–19 (2020)

Active efflux of antibiotics preventing their accumulation to toxic intracellular concentrations contributes to clinically relevant multidrug resistance. Inhibition of active efflux potentiates antibiotic activity, indicating that efflux inhibitors could be used in combination with antibiotics to reverse drug resistance. Expression of ramA by Salmonella enterica serovar Typhimurium increases in response to efflux inhibition, irrespective of the mode of inhibition. […]