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Success Stories


Publications
Alexidine Dihydrochloride Has Broad-Spectrum Activities against Diverse Fungal Pathogens

mspher

Mamouei Z, Alqarihi A, Singh S, Xu S, Mansour MK, Ibrahim AS
mspher - vol. 3 1-11 (2018)

Publications
Amodiaquine improves insulin resistance and lipid metabolism in diabetic model mice

Diabetes Obes Metab.

Jung H, Park S, Hee S, Lee D, Lee I, Kim M, Jeong Y, Hee Y, Bs L
Diabetes Obes Metab. 1-14 (2018)

Publications
Antimicrobial and Antibiofilm Activity of Synergistic Combinations of a Commercially Available Small Compound Library With Colistin Against Pseudomonas aeruginosa

Frontiers in Micro

Torres NS, Montelongo-jauregui D, Abercrombie JJ, Srinivasan A, Lopez-ribot JL, Ramasubramanian AK
Frontiers in Micro - vol. 9 1-12 (2018)

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 […]

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
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
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
The 2019 Garrod Lecture: MDR efflux in Gram-negative bacteria – How understanding resistance led to a new tool for drug discovery

Journal of Antimicrobial Chemotherapy

Piddock LJ
Journal of Antimicrobial Chemotherapy - vol. 74 3128-3134 (2019)

The AcrAB-TolC MDR efflux system confers intrinsic MDR and overproduction confers clinically relevant resistance to some antibiotics active against Gram-negative bacteria. The system is made up of three components, namely AcrA, AcrB and TolC, otherwise known as the AcrAB-TolC tripartite system. Inactivation or deletion of a gene encoding one of the constituent proteins, or substitution […]

Publications
A Small Molecule Targeting Mutagenic Translesion

Cell

Wojtaszek JL, Chatterjee N, Najeeb J, Hong J, Walker GC, Zhou P
Cell - vol. 178 152-159.e11 (2019)