Article-Journal

A simple and fuzzy method to align and compare druggable ligand-binding sites

A novel method to measure distances between druggable protein cavities is presented.

Schalon, C.

Identification of Nonpeptide CCR5 Receptor Agonists by Structure-based Virtual Screening

A three-dimensional model of the chemokine receptor CCR5 has been built to fulfill structural peculiarities of its α-helix bundle and to distinguish known CCR5 antagonists from …

Kellenberger, E.

Topological analysis of the complex formed between neurokinin A and the NK2 tachykinin receptor

Neurokinin A stimulates physiological responses in the peripheral and central nervous systems upon interacting primarily with the tachykinin NK2 receptor (NK2R).

Zoffmann, S.

Optimizing Fragment and Scaffold Docking by Use of Molecular Interaction Fingerprints

Protein−ligand interaction fingerprints have been used to postprocess docking poses of three ligand data sets:  a set of 40 low-molecular-weight compounds from the Protein Data …

Marcou, G.

Chemogenomic approaches to rational drug design

Paradigms in drug design and discovery are changing at a significant pace.

Rognan, D.

In Silico-Guided Target Identification of a Scaffold-Focused Library:  1,3,5-Triazepan-2,6-diones as Novel Phospholipase A2 Inhibitors

A collection of 2150 druggable active sites from the Protein Data Bank was screened by high-throughput docking to identify putative targets for five representative molecules of a …

Muller, P.

Redesign of Schistosoma mansoni NAD+ Catabolizing Enzyme: Active Site H103W Mutation Restores ADP-Ribosyl Cyclase Activity

Schistosoma mansoni NAD(P)+ catabolizing enzyme (SmNACE) is a new member of the ADP-ribosyl cyclase family.

Kuhn, I.

Identification and characterisation of the dopamine receptor II from the cat flea Ctenocephalides felis (CfDopRII)

G protein-coupled receptors (GPCRs) represent a protein family with a wide range of functions.

Gerber, S.

N-Benzoyl-N-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes: Development of 4-Chlorophenylcarboxamide (Calhex 231) as a New Calcium Sensing Receptor Ligand Demonstrating Potent Calcilytic Activity

A structure−activity relationship (SAR) study was performed principally at the N1 position of N1-arylsulfonyl-N2-[1-(1-naphthyl)ethyl]-trans-1,2-diaminocyclohexanes, a new family …

Kessler, A.