Rognan, D.

Targeting undruggable carbohydrate recognition sites through focused fragment library design.

Carbohydrate-protein interactions are key for cell-cell and host-pathogen recognition and thus, emerged as viable therapeutic targets.

Shanina, E.

High-Throughput Screening for Extracellular Inhibitors of the FLT3 Receptor Tyrosine Kinase Reveals Chemically Diverse and Druggable Negative Allosteric Modulators.

Inhibiting receptor tyrosine kinases is commonly achieved by two main strategies targeting either the intracellular kinase domain by low molecular weight compounds or the …

Hany, R.

Targeting the Central Pocket of the Pseudomonas aeruginosa Lectin LecA.

Pseudomonas aeruginosa is an opportunistic ESKAPE pathogen that produces two lectins, LecA and LecB, as part of its large arsenal of virulence factors.

Siebs, E.

Unexpected similarity between HIV-1 reverse transcriptase and tumor necrosis factor binding sites revealed by computer vision.

Rationalizing the identification of hidden similarities across the repertoire of druggable protein cavities remains a major hurdle to a true proteome-wide structure-based …

Eguida, M.

True Accuracy of Fast Scoring Functions to Predict High-Throughput Screening Data from Docking Poses: The Simpler the Better.

Hundreds of fast scoring functions have been developed over the last 20 years to predict binding free energies from three-dimensional structures of protein-ligand complexes.

Tran-Nguyen, V.

Non-Carbohydrate Glycomimetics as Inhibitors of Calcium(II)-Binding Lectins.

Because of the antimicrobial resistance crisis, lectins are considered novel drug targets.

Kuhaudomlarp, S.

Design, Synthesis and Biological Evaluation of Arylpyridin-2-yl Guanidine Derivatives and Cyclic Mimetics as Novel MSK1 Inhibitors. An Application in an Asthma Model.

Mitogen- and Stress-Activated Kinase 1 (MSK1) is a nuclear kinase, taking part in the activation pathway of the pro-inflammatory transcription factor NF-kB and is demonstrating a …

Bollenbach, M.

A Computer Vision Approach to Align and Compare Protein Cavities: Application to Fragment-Based Drug Design.

Identifying local similarities in binding sites from distant proteins is a major hurdle to rational drug design.

Eguida, M.

Benchmarking Data Sets from PubChem BioAssay Data: Current Scenario and Room for Improvement.

Developing realistic data sets for evaluating virtual screening methods is a task that has been tackled by the cheminformatics community for many years.

Tran-Nguyen, V.

LIT-PCBA: An Unbiased Data Set for Machine Learning and Virtual Screening

Comparative evaluation of virtual screening methods requires a rigorous benchmarking procedure on diverse, realistic, and unbiased data sets.

Tran-Nguyen, V.