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.
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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.
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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.
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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.
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Chemogenomic approaches to rational drug design

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

Rognan, D.
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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.
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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.
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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.
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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.
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