Publications


Publications
Bioinformatics analysis of high-throughput data to validate potential novel biomarkers and small molecule drugs for glioblastoma multiforme

Journal of International Medical Research

Qi F, Li Q, Lu X, Chen Z
Journal of International Medical Research - vol. 48 1-17 (2020)

Objective: There have been no recent improvements in the glioblastoma multiforme (GBM) outcome, with median survival remaining 15 months. Consequently, the need to identify novel biomarkers for GBM diagnosis and prognosis, and to develop targeted therapies is high. This study aimed to establish biomarkers for GBM pathogenesis and prognosis. Methods: In total, 220 overlapping differentially […]

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
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 […]

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
First-in-class allosteric inhibitors of bacterial IMPDHs

European Journal of Medicinal Chemistry

Alexandre T, Lupan A, Helynck O, Vichier-Guerre S, Dugué L, Gelin M, Haouz A, Labesse G, Munier-Lehmann H
European Journal of Medicinal Chemistry - vol. 167 124-132 (2019)

Inosine-5‘-monophosphate dehydrogenase (IMPDH) is an essential enzyme in many bacterial pathogens and is considered as a potential drug target for the development of new antibacterial agents. Our recent work has revealed the crucial role of one of the two structural domains (i.e. Bateman domain) in the regulation of the quaternary structure and enzymatic activity of […]

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
Metabolomics-Driven Exploration of the Chemical Drug Space to Predict Combination Antimicrobial Therapies

Molecular Cell

Campos AI, Zampieri M
Molecular Cell - vol. 74 1291-1303.e6 (2019)

Alternative to the conventional search for single-target, single-compound treatments, combination therapies can open entirely new opportunities to fight antibiotic resistance. However, combinatorial complexity prohibits experimental testing of drug combinations on a large scale, and methods to rationally design combination therapies are lagging behind. Here, we developed a combined experimental-computational approach to predict drug-drug interactions using […]

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
Identification of Off-Patent Compounds That Present Antifungal Activity against the Emerging Fungal Pathogen Candida auris

Frontiers in Cellular and Infection Microbiology

De Oliveira HC, Monteiro MC, Rossi SA, Pemán J, Ruiz-Gaitán A, Mendes-Giannini MJS, Mellado E, Zaragoza O
Frontiers in Cellular and Infection Microbiology - vol. 9 1-10 (2019)

Candida auris is an emerging fungal pathogen of great concern among the scientific community because it is causing an increasing number of hospital outbreaks of difficult management worldwide. In addition, isolates from this species frequently present reduced susceptibility to azole and echinocandin drugs. For this reason, it is necessary to develop new antifungal strategies to […]

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 […]