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Drug Evaluation, Preclinical

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Integration of virtual screening and susceptibility test to discover active-site subpocket-specific biogenic inhibitors of Helicobacter pylori shikimate dehydrogenase.

International microbiology : the official journal of the Spanish Society for Microbiology
Shikimate dehydrogenase (HpSDH) (EC 1.1.1.25) is a key enzyme in the shikimate pathway of Helicobacter pylori (H. pylori), which catalyzes the NADPH-dependent reversible reduction of 3-dehydroshikimate to shikimate. Targeting HpSDH has been recognize...

RASPELD to Perform High-End Screening in an Academic Environment toward the Development of Cancer Therapeutics.

ChemMedChem
The identification of compounds for dissecting biological functions and the development of novel drug molecules are central tasks that often require screening campaigns. However, the required architecture is cost- and time-intensive. Herein we descri...

Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HTR Ligands.

Molecules (Basel, Switzerland)
The identification of subtype-selective GPCR (G-protein coupled receptor) ligands is a challenging task. In this study, we developed a computational protocol to find compounds with 5-HTR versus 5-HTR selectivity. Our approach employs the hierarchical...

Agonists of G-Protein-Coupled Odorant Receptors Are Predicted from Chemical Features.

The journal of physical chemistry letters
Predicting the activity of chemicals for a given odorant receptor is a longstanding challenge. Here the activity of 258 chemicals on the human G-protein-coupled odorant receptor (OR)51E1, also known as prostate-specific G-protein-coupled receptor 2 (...

Virtual screening by a new Clustering-based Weighted Similarity Extreme Learning Machine approach.

PloS one
Machine learning techniques are becoming popular in virtual screening tasks. One of the powerful machine learning algorithms is Extreme Learning Machine (ELM) which has been applied to many applications and has recently been applied to virtual screen...

Antifungal activities against toxigenic Fusarium specie and deoxynivalenol adsorption capacity of ion-exchanged zeolites.

Journal of environmental science and health. Part. B, Pesticides, food contaminants, and agricultural wastes
Zeolites are often used as adsorbents materials and their loaded cations can be exchanged with metal ions in order to add antimicrobial properties. The aim of this study was to use the 4A zeolite and its derived ion-exchanged forms with Zn, Li, Cu an...

α-glucosidase inhibitors isolated from L.

Natural product research
The aim of the study was to isolate digestive enzymes inhibitors from through a bioassay-guided fractionation approach. Repeated silica gel and sephadex LH 20 column chromatographies of bioactive fractions afforded stigmasterol, quercetin and avicul...

Antiviral activity of aconite alkaloids from Debx.

Natural product research
Four diterpenoid alkaloids, namely, () hypaconitine, ) songorine, () mesaconitine and () aconitine, were isolated from the ethanol root extract of Debx. The antiviral activities of these alkaloids against tobacco mosaic virus (TMV) and cucumber mosa...

Commercial glucometer as signal transducer for simple evaluation of DNA methyltransferase activity and inhibitors screening.

Analytica chimica acta
DNA methyltransferase (MTase) plays an important role in many biological processes and has been recognized as a predictive cancer biomarker far before other signs of malignancy and a therapeutic target in cancer treatment. Thus simple and sensitive d...