Chemical Biology & Drug Design
© John Wiley & Sons A/S. Published by John Wiley & Sons Ltd
Edited By: David Selwood
Impact Factor: 2.282
ISI Journal Citation Reports © Ranking: 2011: 30/59 (Chemistry Medicinal); 182/290 (Biochemistry & Molecular Biology)
Online ISSN: 1747-0285
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Recently Published Articles
- Rationally Designed Sulfamides As Glutamate Carboxypeptidase II (GCPII) Inhibitors
Cindy J. Choy, Melody D. Fulton, Austen L. Davis, Mark Hopkins, Joseph K. Choi, Marc O. Anderson and Clifford E. Berkman
Accepted manuscript online: 17 JUN 2013 06:26AM EST | DOI: 10.1111/cbdd.12174
This current study explores a new class of GCP II inhibitors, glutamyl sulfamides, which possess a neutral tetrahedral zinc-binding motif. A small library containing 6 sulfamides was prepared and evaluated for inhibitory potency against purified GCPII. While most inhibitors have potencies in the micromolar range, one showed promising sub-micromolar potency, with the optimal inhibitor in this series being aspartyl-glutamyl sulfamide
- Evaluation of the efficiency of synthesized efflux pump inhibitors on Salmonella enterica ser. Typhimurium cells
Simona Sutkuvienė, Valeryia Mikalayeva, Silvia Pavan, Federico Berti and Rimantas Daugelavičius
Accepted manuscript online: 13 JUN 2013 09:46AM EST | DOI: 10.1111/cbdd.12173
This study was focused on the evaluation of efficiency of synthesized resistance-nodulation-division (RND) family efflux pump inhibitors. Efficiency of the synthesized compounds was investigated on Salmonella enterica ser. Typhimurium cells using electrochemical and spectrofluorimetric methods. The results obtained showed that the registered efficiency of inhibitors depends on the permeability of cell outer membrane and the method of assay used.
- Evaluating the predictivity of virtual screening for Abl kinase inhibitors to hinder drug resistance
Osman A B S M Gani, Dilip Narayanan and Richard A. Engh
Accepted manuscript online: 8 JUN 2013 07:12AM EST | DOI: 10.1111/cbdd.12170
Virtual screenings were performed on ABL1 kinase to study inhibitors for wild type T315 mutant form. In addition, chemoinformatic methods were also applied on kinase inhibitors. We show that VS and ligand-based studies are complementary in understanding the features that should be considered during in silico studies.
- TAK1 Inhibition in theDFG-Out Conformation
Iain Kilty, Martin P. Green, Andrew S. Bell, David G. Brown, Peter G. Dodd, Christopher Hewson, Samantha J. Hughes, Christopher Phillips, Thomas Ryckmans, Robert T. Smith, Willem P. van Hoorn, Philip Cohen and Lyn H. Jones
Accepted manuscript online: 7 JUN 2013 11:26AM EST | DOI: 10.1111/cbdd.12169
The first example of an inhibitor of the kinase TAK1 that binds in the DFG-out conformation is disclosed. These preliminary studies used kinase-targeted screening and structure-based drug design to create a molecule with dual pharmacological inhibition of p38 and TAK1 that demonstrated significant activity in a cell-based, anti-inflammatory assay.
- Preptin Analogues: Chemical Synthesis, Secondary Structure and Biological Studies
Christina M. Buchanan, Zhenzhen Peng, Aiko Cefre and Vijayalekshmi Sarojini
Accepted manuscript online: 7 JUN 2013 11:26AM EST | DOI: 10.1111/cbdd.12168
Preptin analogues with non-protein amino acids have been chemically synthesized, characterized and analysed for their ability ability to augment insulin secretion from βTC6-F7 β-cells.