Protein Binding

On the Difficulty to Rescore Hits from Ultralarge Docking Screens.

Docking-based virtual screening tools customized to mine ultralarge chemical spaces are consistently reported to yield both higher hit rates and more potent ligands than that …

Sindt, F.

Large scale investigation of GPCR molecular dynamics data uncovers allosteric sites and lateral gateways.

G protein-coupled receptors (GPCRs) constitute a functionally diverse protein family and are targets for a broad spectrum of pharmaceuticals.

Aranda-García, D.

CACHE Challenge #1: Targeting the WDR Domain of LRRK2, A Parkinson's Disease Associated Protein.

The CACHE challenges are a series of prospective benchmarking exercises to evaluate progress in the field of computational hit-finding.

Li, F.

Subpocket Similarity-Based Hit Identification for Challenging Targets: Application to the WDR Domain of LRRK2.

We herewith applied a priori a generic hit identification method (POEM) for difficult targets of known three-dimensional structure, relying on the simple knowledge of …

Eguida, M.

Benchmarking AlphaFold-Generated Structures of Chemokine-Chemokine Receptor Complexes.

AlphaFold and AlphaFold-Multimer have become two essential tools for the modeling of unknown structures of proteins and protein complexes.

Urvas, L.

Structural Insights into Molecular Recognition and Receptor Activation in Chemokine-Chemokine Receptor Complexes.

The chemokine system is a key player in the functioning of the immune system and a sought-after target for drug candidates.

Urvas, L.

Estimating the Similarity between Protein Pockets.

With the exponential increase in publicly available protein structures, the comparison of protein binding sites naturally emerged as a scientific topic to explain observations or …

Eguida, M.

On the Frustration to Predict Binding Affinities from Protein-Ligand Structures with Deep Neural Networks.

Accurate prediction of binding affinities from protein-ligand atomic coordinates remains a major challenge in early stages of drug discovery.

Volkov, M.

Modeling of CCR5 Recognition by HIV-1 gp120: How the Viral Protein Exploits the Conformational Plasticity of the Coreceptor.

The chemokine receptor CCR5 is a key player in HIV-1 infection.

Jacquemard, C.

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.