Publications


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, […]

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
High Content Screening Using New U2OS Reporter Cell Models Identifies Harmol Hydrochloride as a Selective and Competitive Antagonist of the Androgen Receptor

Cells

Dellal H, Boulahtouf A, Alaterre E, Cuenant A, Grimaldi M, Bourguet W, Gongora C, Balaguer P, Pourquier P
Cells - vol. 9 (2020)

Prostate cancer is the most commonly diagnosed malignancy in men. Its growth mainly relies on the activity of the androgen receptor (AR), justifying the use of androgen deprivation therapy as a gold standard treatment for the metastatic disease. Inhibition of the androgen axis using second generation antagonists has improved patients’ survival, but is systematically confronted […]

Publications
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

Journal of Pathology, Microbiology and Immunology

Foerster S, Gustafsson TN, Brochado AR, Desilvestro V, Typas A, Unemo M
Journal of Pathology, Microbiology and Immunology - vol. 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
Identification of repositionable drugs with novel antimycotic activity by screening the Prestwick Chemical Library against emerging invasive moulds

Journal of Global Antimicrobial Resistance

Yousfi H, Ranque S, Cassagne C, Rolain JM, Bittar F
Journal of Global Antimicrobial Resistance - vol. 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 […]

Publications
High content drug screening for Fanconi anemia therapeutics

Orphanet Journal of Rare Diseases

Montanuy H, Camps-Fajol C, Camps-Fajol C, Carreras-Puigvert J, Carreras-Puigvert J, Carreras-Puigvert J, Häggblad M, Häggblad M, Lundgren B, Aza-Carmona M, Aza-Carmona M, Helleday T, Minguillón J, Minguillón J, Minguillón J, Surrallés J, Surrallés J, Surrallés J, Surrallés J
Orphanet Journal of Rare Diseases - vol. 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
Drosophila SMN2 minigene reporter model identifies moxifloxacin as a candidate therapy for SMA

FASEB Journal

Konieczny P, Artero R
FASEB Journal - vol. 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
New multidrug efflux inhibitors for gram-negative bacteria

mBio

Marshall RL, Lloyd GS, Lawler AJ, Element SJ, Kaur J, Ciusa ML, Ricci V, Tschumi A, Kühne H, Alderwick LJ, Piddock LJ
mBio - vol. 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 […]

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 […]