Publications


Publications
Exploring the Human Cytomegalovirus Core Nuclear Egress Complex as a Novel Antiviral Target: A New Type of Small Molecule Inhibitors

Alkhashrom S, Kicuntod J, Häge S, Schweininger J, Muller YA, Lischka P, Marschall M, Eichler J.
Viruses 471 (2021)

Nuclear egress is an essential process in the replication of human cytomegalovirus (HCMV), as it enables the migration of newly formed viral capsids from the nucleus into the cytoplasm. Inhibition of the HCMV core nuclear egress complex (core NEC), composed of viral proteins pUL50 and pUL53, has been proposed as a potential new target for […]

Publications
A fluorescence-based high throughput-screening assay for the SARS-CoV RNA synthesis complex

Journal of Virological Methods

Eydoux C, Fattorini V, Shannon A, Le TTN, Didier B, Canard B, Guillemot JC
Journal of Virological Methods - vol. 288 114013 (2021)

The Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV) emergence in 2003 introduced the first serious human coronavirus pathogen to an unprepared world. To control emerging viruses, existing successful anti(retro)viral therapies can inspire antiviral strategies, as conserved viral enzymes (eg., viral proteases and RNA-dependent RNA polymerases) represent targets of choice. Since 2003, much effort has been expended […]

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
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
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
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
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 […]