Rognan, D.

Structure-Based Approaches to Target Fishing and Ligand Profiling

Chemogenomics is an emerging interdisciplinary field aiming at identifying all possible ligands of all possible targets.

Rognan, D.

Estrogen Receptor Alpha as a Key Target of Red Wine Polyphenols Action on the Endothelium

Background A greater reduction in cardiovascular risk and vascular protection associated with diet rich in polyphenols are generally accepted; however, the molecular targets for …

Chalopin, M.

Increasing Selectivity of CC Chemokine Receptor 8 Antagonists by Engineering Nondesolvation Related Interactions with the Intended and Off-Target Binding Sites

The metabolic stability and selectivity of a series of CCR8 antagonists against binding to the hERG ion channel and cytochrome Cyp2D6 are studied by principal component analysis.

Shamovsky, I.

Molecular determinants of non-competitive antagonist binding to the mouse GPRC6A receptor

GPRC6A displays high sequence homology to the Ca2+-sensing receptor (CaSR).

Faure, H.

Stereospecificity of the Siderophore Pyochelin Outer Membrane Transporters in Fluorescent Pseudomonads

Pyochelin (Pch) and enantio-pyochelin (EPch) are enantiomer siderophores that are produced by Pseudomonas aeruginosa and Pseudomonas fluorescens, respectively, under iron …

Hoegy, F.

Development and Validation of a Novel Protein−Ligand Fingerprint To Mine Chemogenomic Space: Application to G Protein-Coupled Receptors and Their Ligands

The present study introduces a novel low-dimensionality fingerprint encoding both ligand and target properties which is suitable to mine protein−ligand chemogenomic space.

Weill, N.

Conformationally constrained opioid ligands: The Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold

Replacement of the constrained phenylalanine analogue 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) in the opioid Dmt-Tic-Gly-NH-Bn scaffold by the …

Ballet, S.

Customizing G Protein-coupled receptor models for structure-based virtual screening.

This review will focus on the construction, refinement, and validation of G Protein-coupled receptor models for the purpose of structure-based virtual screening.

De Graaf, C.

Selective Structure-Based Virtual Screening for Full and Partial Agonists of the β2 Adrenergic Receptor

The recently solved high-resolution X-ray structure of the β2 adrenergic receptor has been challenged for its ability to discriminate inverse agonists/antagonists from partial/full …

De Graaf, C.

Hot-Spots-Guided Receptor-Based Pharmacophores (HS-Pharm): A Knowledge-Based Approach to Identify Ligand-Anchoring Atoms in Protein Cavities and Prioritize Structure-Based Pharmacophores

The design of biologically active compounds from ligand-free protein structures using a structure-based approach is still a major challenge.

Barillari, C.