Benzohydrazide and Phenylacetamide Scaffolds: New Putative ParE Inhibitors

Tricyclic GyrB/ParE (TriBE) Inhibitors: A New Class of Broad-Spectrum Dual-Targeting Antibacterial Agents

Increasing resistance to every major class of antibiotics and a dearth of novel classes of antibacterial agents in development pipelines has created a dwindling reservoir of treatment options for serious bacterial infections. The bacterial type IIA topoisomerases, DNA gyrase and topoisomerase IV, are validated antibacterial drug targets with multiple prospective drug binding sites, including th...

El Pare

EL PARE Com que vivia a Batignolles i treballava al ministeri d’Instrucció Pública, cada dia agafava l’òmnibus per anar fins al despatx. I cada matí feia el trajecte fins al centre de París, davant una noia de qui es va enamorar. Ella anava a la seva botiga, cada dia, a la mateixa hora. Era una moreneta menuda, d’aquestes brunes que tenen els ulls tan negres que semblen taques i un color de car...

Selective Immunoproteasome Inhibitors with Non-Peptide Scaffolds

Bacterial toxin inhibitors based on multivalent scaffolds.

Protein toxins released by certain intestinal bacteria are the cause of many diarrhoeal diseases including cholera and travellers' diarrhoea. The toxins enter their target cells by first binding to specific glycolipids in the cell membrane. Inhibition of these protein-carbohydrate interactions has the potential to prevent the toxins from reaching their site of action, and thus avoid the ensuing...

Structure- and Ligand-Based Virtual Screening Identifies New Scaffolds for Inhibitors of the Oncoprotein MDM2

A major challenge in the field of ligand discovery is to identify chemically useful fragments that can be developed into inhibitors of specific protein-protein interactions. Low molecular weight fragments (with molecular weight less than 250 Da) are likely to bind weakly to a protein's surface. Here we use a new virtual screening procedure which uses a combination of similarity searching and do...