Archives des Publications - Page 9 sur 46 - Prestwick Chemical Libraries

Publications

Utilisation of the Prestwick Chemical Library to identify drugs that inhibit the growth of mycobacteria

PLoS ONE

Kanvatirth P, Jeeves RE, Bacon J, Besra GS, Alderwick LJ
PLoS ONE - vol. 14 (2019)

Tuberculosis (TB) is an infectious bacterial disease that kills approximately 1.3 million people every year. Despite global efforts to reduce both the incidence and mortality associated with TB, the emergence of drug resistant strains has slowed any progress made towards combating the spread of this deadly disease. The current TB drug regimen is inadequate, takes […]

Publications

Identification and characterization of menadione and benzethonium chloride as potential treatments of Pierce’s disease of grapevines

Phytopathology

Zhang S, Jain M, Fleites LA, Rayside PA, Gabriel DW
Phytopathology - vol. 109 233-239 (2019)

Xylella fastidiosa infects a wide range of plant hosts and causes Pierce’s disease (PD) of grapevines. The type 1 multidrug resistance (MDR) efflux system is essential for pathogenicity and survival of bacterial pathogens in planta. X. fastidiosa, with a single MDR system, is significantly more vulnerable to inhibition by small-molecule treatments than most bacterial pathogens […]

Publications

Screening and evaluation of antiviral compounds against Equid alpha-herpesviruses using an impedance-based cellular assay

Virology

Thieulent CJ, Hue ES, Fortier CI, Dallemagne P, Zientara S, Munier-Lehmann H, Hans A, Fortier GD, Pitel PH, Vidalain PO, Pronost SL
Virology - vol. 526 105-116 (2019)

Equid alpha-herpesviruses (EHV) are responsible for different diseases in equine population. EHV-1 causes respiratory diseases, abortions and nervous disorders, EHV-4 causes respiratory diseases and sporadic abortion, while EHV-3 is responsible of equine coital exanthema. In view of the lack of efficacy of vaccines against EHV-1 and EHV-4 and in the absence of vaccines against EHV-3, […]

Publications

Drug‐induced increase in lysobisphosphatidic acid reduces the cholesterol overload in Niemann–Pick type C cells and mice

EMBO reports

Moreau D, Vacca F, Vossio S, Scott C, Colaco A, Paz Montoya J, Ferguson C, Damme M, Moniatte M, Parton RG, Platt FM, Gruenberg J
EMBO reports - vol. 20 1-15 (2019)

Most cells acquire cholesterol by endocytosis of circulating low-density lipoproteins (LDLs). After cholesteryl ester de-esterification in endosomes, free cholesterol is redistributed to intracellular membranes via unclear mechanisms. Our previous work suggested that the unconventional phospholipid lysobisphosphatidic acid (LBPA) may play a role in modulating the cholesterol flux through endosomes. In this study, we used the […]

Publications

Fibrates as drugs with senolytic and autophagic activity for osteoarthritis therapy

EBioMedicine

Nogueira-Recalde U, Lorenzo-Gómez I, Blanco FJ, Loza MI, Grassi D, Shirinsky V, Shirinsky I, Lotz M, Robbins PD, Domínguez E, Caramés B
EBioMedicine - vol. 45 588-605 (2019)

Background: Ageing-related failure of homeostasis mechanisms contributes to articular cartilage degeneration and osteoarthritis (OA), for which disease-modifying treatments are not available. Our objective was to identify molecules to prevent OA by regulating chondrocyte senescence and autophagy. Methods: Human chondrocytes with IL-6 induced senescence and autophagy suppression and SA-β-gal as a reporter of senescence and LC3 […]

Publications

A yeast-based screening assay identifies repurposed drugs that suppress mitochondrial fusion and mtDNA maintenance defects

DMM Disease Models and Mechanisms

Delerue T, Tribouillard-Tanvier D, Daloyau M, Khosrobakhsh F, Emorine LJ, Friocourt G, Belenguer P, Blondel M, Arnauné-Pelloquin L
DMM Disease Models and Mechanisms - vol. 12 1-9 (2019)

Mitochondria continually move, fuse and divide, and these dynamics are essential for the proper function of the organelles. Indeed, the dynamic balance of fusion and fission of mitochondria determines their morphology and allows their immediate adaptation to energetic needs as well as preserving their integrity. As a consequence, mitochondrial fusion and fission dynamics and the […]

Publications

Approved drugs screening against the nsP1 capping enzyme of Venezuelan equine encephalitis virus using an immuno-based assay

Antiviral Research

Ferreira-Ramos AS, Li C, Eydoux C, Contreras JM, Morice C, Quérat G, Gigante A, Pérez Pérez MJ, Jung ML, Canard B, Guillemot JC, Decroly E, Coutard B
Antiviral Research - vol. 163 59-69 (2019)

Alphaviruses such as the Venezuelan equine encephalitis virus (VEEV) are important human emerging pathogens transmitted by mosquitoes. They possess a unique viral mRNA capping mechanism catalyzed by the viral non-structural protein nsP1, which is essential for virus replication. The alphaviruses capping starts by the methylation of a GTP molecule by the N7-guanine methyltransferase (MTase) activity; […]

Publications

Evaluation of a library of FDA-approved drugs for their ability to potentiate antibiotics against multidrug-resistant gram-negative pathogens

Antimicrobial Agents and Chemotherapy

Hind CK, Dowson CG, Sutton JM, Jackson T, Clifford M, Garner RC, Czaplewski L
Antimicrobial Agents and Chemotherapy - vol. 63 1-6 (2019)

The Prestwick library was screened for antibacterial activity or « antibiotic resistance breaker » (ARB) potential against four species of Gram-negative pathogens. Discounting known antibacterials, the screen identified very few ARB hits, which were strain/drug specific. These ARB hits included antimetabolites (zidovudine, floxuridine, didanosine, and gemcitabine), anthracyclines (daunorubicin, mitoxantrone, and epirubicin), and psychoactive drugs (gabapentin, fluspirilene, and […]

Publications

A New Model of Sensorial Neuron-Like Cells for HTS of Novel Analgesics for Neuropathic Pain

SLAS Discovery

Martínez AL, Brea J, Monroy X, Merlos M, Burgueño J, Loza MI
SLAS Discovery - vol. 24 158-168 (2019)

In this study we developed a new translational phenotypic in vitro model for high-throughput screening (HTS) of novel analgesics for treating neuropathic pain, in order to address the poor translation of traditional recombinant models. The immortalized dorsal root ganglia (DRG) neuron-like F11 cell line was selected based on its phenotype after differentiation. The acquisition of […]

Publications

Guanabenz acetate induces endoplasmic reticulum stress-related cell death in hepatocellular carcinoma cells

Journal of Pathology and Translational Medicine

Kang HJ, Seol HS, Lee SE, Suh YA, Kim J, Jang SJ, Yu E
Journal of Pathology and Translational Medicine - vol. 53 94-103 (2019)

Background: Development of chemotherapeutics for the treatment of advanced hepatocellular carcinoma (HCC) has been lagging. Screening of candidate therapeutic agents by using patient-derived preclinical models may facilitate drug discovery for HCC patients. Methods: Four primary cultured HCC cells from surgically resected tumor tissues and six HCC cell lines were used for high-throughput screening of 252 […]

All our screening libraries