Rognan, D.

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.

An anti-virulence drug targeting the evolvability protein Mfd protects against infections with antimicrobial resistant ESKAPE pathogens.

The increasing incidence of antibiotic resistance and the decline in the discovery of novel antibiotics have resulted in a global health crisis, particularly, for the treatment of …

Tran, S.

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.

FLT3 signaling inhibition abrogates opioid tolerance and hyperalgesia while preserving analgesia.

Navigating the duality of opioids' potent analgesia and side effects, including tolerance and hyperalgesia, is a significant challenge in chronic pain management, often prompting …

Jouvenel, A.

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.

Protein Structure-Based Organic Chemistry-Driven Ligand Design from Ultralarge Chemical Spaces.

Ultralarge chemical spaces describing several billion compounds are revolutionizing hit identification in early drug discovery.

Sindt, F.

Overlap of On-demand Ultra-large Combinatorial Spaces with On-the-shelf Drug-like Libraries.

On-demand combinatorial spaces are shifting paradigms in early drug discovery, by considerably increasing the searchable chemical space to several billions of compounds while …

Perebyinis, M.

Target-Focused Library Design by Pocket-Applied Computer Vision and Fragment Deep Generative Linking.

We here describe a computational approach (POEM: Pocket Oriented Elaboration of Molecules) to drive the generation of target-focused libraries while taking advantage of all …

Eguida, M.

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.