Publications

Publications
Sanguinarine Inhibits the 2-Ketogluconate Pathway of Glucose Utilization in Pseudomonas Aeruginosa

 Falchi, F. A.; Borlotti, G.; Ferretti, F.; Pellegrino, G.; Raneri, M.; Schiavoni, M.; Caselli, A.; Briani, F.
 Front Microbiol 12, 744458 (2021)

Interfering with the ability of pathogenic bacteria to import glucose may represent a new promising antibacterial strategy, especially for the treatment of infections occurring in diabetic and other hyperglycemic patients. Such patients are particularly susceptible to infections caused by a variety of bacteria, among which opportunistic pathogens like Pseudomonas aeruginosa. In P. aeruginosa, glucose can […]

Publications
High-Throughput Screening of TRPV1 Ligands in the Light of the Bioluminescence Resonance Energy Transfer Technique

 Chappe, Y.; Michel, P.; Joushomme, A.; Barbeau, S.; Pierredon, S.; Baron, L.; Garenne, A.; Gannes, F. P. D.; Hurtier, A.; Mayer, S.; Lagroye, I.; Quignard, J.-F.; Ducret, T.; Compan, V.; Franchet, C.; Percherancier, Y.
 Mol Pharmacol 100 (3), 237–257 (2021)

Ion channels are attractive drug targets for many therapeutic applications. However, high-throughput screening (HTS) of drug candidates is difficult and remains very expensive. We thus assessed the suitability of the bioluminescence resonance energy transfer (BRET) technique as a new HTS method for ionchannel studies by taking advantage of our recently characterized intra- and intermolecular BRET […]

Publications
Isoconazole and Clemizole Hydrochloride Partially Reverse the Xeroderma Pigmentosum C Phenotype

 Kobaisi, F.; Sulpice, E.; Barette, C.; Fayyad, N.; Fauvarque, M.-O.; Badran, B.; Fayyad-Kazan, M.; Fayyad-Kazan, H.; Gidrol, X.; Rachidi, W.
 Int J Mol Sci 22 (15) (2021)

Xeroderma Pigmentosum protein C (XPC) is involved in recognition and repair of bulky DNA damage such as lesions induced by Ultra Violet (UV) radiation. XPC-mutated cells are, therefore, photosensitive and accumulate UVB-induced pyrimidine dimers leading to increased cancer incidence. Here, we performed a high-throughput screen to identify chemicals capable of normalizing the XP-C phenotype (hyper-photosensitivity […]

Publications
Identification of Harmine and β-Carboline Analogs from a High-Throughput Screen of an Approved Drug Collection; Profiling as Differential Inhibitors of DYRK1A and Monoamine Oxidase A and for in Vitro and in Vivo Anti-Cancer Studies

 Tarpley, M.; Oladapo, H. O.; Strepay, D.; Caligan, T. B.; Chdid, L.; Shehata, H.; Roques, J. R.; Thomas, R.; Laudeman, C. P.; Onyenwoke, R. U.; Darr, D. B.; Williams, K. P.
 European Journal of Pharmaceutical Sciences 162, 105821 (2021)

DYRK1A (dual-specificity tyrosine phosphorylation-regulated kinase 1a) is highly expressed in glioma, an aggressive brain tumor, and has been proposed as a therapeutic target for cancer. In the current study, we have used an optimized and validated time-resolved fluorescence energy transfer (TR-FRET)-based DYRK1A assay for high-throughput screening (HTS) in 384-well format. A small-scale screen of the […]

Publications
Inhibition of Iduronic Acid Biosynthesis by Ebselen Reduces Glycosaminoglycan Accumulation in Mucopolysaccharidosis Type I Fibroblasts

 Maccarana, M.; Tykesson, E.; Pera, E. M.; Gouignard, N.; Fang, J.; Malmström, A.; Ghiselli, G.; Li, J.
 Glycobiology 31 (10), 1319–1329 (2021)

Mucopolysaccharidosis type I (MPS-I) is a rare lysosomal storage disorder caused by deficiency of the enzyme alpha-L-iduronidase, which removes iduronic acid in both chondroitin/dermatan sulfate (CS/DS) and heparan sulfate (HS) and thereby contributes to the catabolism of glycosaminoglycans (GAGs). To ameliorate this genetic defect, the patients are currently treated by enzyme replacement and bone marrow […]

Publications
Identification of Novel Myelin Repair Drugs by Modulation of Oligodendroglial Differentiation Competence

 Manousi, A.; Göttle, P.; Reiche, L.; Cui, Q.-L.; Healy, L. M.; Akkermann, R.; Gruchot, J.; Schira-Heinen, J.; Antel, J. P.; Hartung, H.-P.; Küry, P.
 EBioMedicine 65, 103276 (2021)

Background: In multiple sclerosis loss of myelin and oligodendrocytes impairs saltatory signal transduction and leads to neuronal loss and functional deficits. Limited capacity of oligodendroglial precursor cells to differentiate into mature cells is the main reason for inefficient myelin repair in the central nervous system. Drug repurposing constitutes a powerful approach for identification of pharmacological […]

Publications
Identification of Lysosome‐targeting Drugs with Anti‐inflammatory Activity as Potential Invasion Inhibitors of Treatment Resistant HER2 Positive Cancers

 Hansen, M. B.; Postol, M.; Tvingsholm, S.; Nielsen, I. Ø.; Dietrich, T. N.; Puustinen, P.; Maeda, K.; Dinant, C.; Strauss, R.; Egan, D.; Jäättelä, M.; Kallunki, T.
 Cell Oncol (Dordr) 44 (4) 805–820 (2019)

Purpose: Most HER2 positive invasive cancers are either intrinsic non-responsive or develop resistance when treated with 1st line HER2 targeting drugs. Both 1st and 2nd line treatments of HER2 positive cancers are aimed at targeting the HER2 receptor directly, thereby strongly limiting the treatment options of HER2/ErbB2 inhibition resistant invasive cancers. Methods: We used phenotypic […]

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
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) […]

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