Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
April 15, 2014
VIP: High-Throughput Screening of Metal–N-Heterocyclic Carbene Complexes against Biofilm Formation by Pathogenic Bacteria
Thierry Bernardi,* Stéphanie Badel, Pascal Mayer, Jérome Groelly, Pierre de Frémont, Béatrice Jacques, Pierre Braunstein, Marie-Laure Teyssot, Christelle Gaulier, Federico Cisnetti, Arnaud Gautier,* Sylvain Roland*
The treatment of certain bacterial infections has become a major public health concern with the increasing emergence of pathogenic bacterial strains that are resistant to most available antibiotics. Alternative strategies to those involving conventional antibiotic treatments are urgently needed to treat these refractory infections. Read more...
Recently Published Articles
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Alycia M. Palmer, Scott J. Burya, Judith C. Gallucci and Prof. Claudia Turro
Article first published online: 17 APR 2014 | DOI: 10.1002/cmdc.201402004
Dual impact with light: cis-H,H-[Rh2(OCCH3NH)2(dppz)(CH3CN)4]2+ exhibits enhanced intercalation and covalent binding to DNA upon activation with visible light. The unique photoinduced dual binding of this complex makes it an attractive photodynamic therapy agent, which may be active against cisplatin-resistant cell lines.
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Dr. Raffaella Amici, Dr. Chiara Bigogno, Dr. Roberto Boggio, Dr. Andrea Colombo, Dr. Stephen M. Courtney, Dr. Roberto Dal Zuffo, Dr. Giulio Dondio, Dr. Fulvia Fusar, Dr. Stefania Gagliardi, Prof. Dr. Saverio Minucci, Dr. Marco Molteni, Dr. Christian A. G. N. Montalbetti, Dr. Annalisa Mortoni, Dr. Mario Varasi, Dr. Stefania Vultaggio and Dr. Ciro Mercurio
Article first published online: 17 APR 2014 | DOI: 10.1002/cmdc.201400037
Problem resolved: A chemical method to resolve the enantiomers of 2-amino-7-[4-fluoro-2-(3-pyridyl)phenyl]-4-methyl-7,8-dihydro-6H-quinazolin-5-one oxime, a Hsp90 inhibitor targeting the N-terminal adenosine triphosphatase site, and the characterization of their inhibitor activity on Hsp90, along with the consequent antiproliferative effect on cancer cells is explored. Pharmacokinetic properties and antitumor activity are also evaluated.
- Investigation of a Vitamin B12 Conjugate as a PET Imaging Probe
Dr. Oluwatayo F. Ikotun, Dr. Bernadette V. Marquez, Dr. Christopher H. Fazen, Dr. Anna R. Kahkoska, Prof. Robert P. Doyle and Prof. Suzanne E. Lapi
Article first published online: 17 APR 2014 | DOI: 10.1002/cmdc.201400048
Co-opting cobalamin: Vitamin B12 is an essential nutrient for all proliferating cells. Rapid proliferation is a common hallmark of cancer; consequently, neoplastic cells have an increased demand for vitamin B12. We exploited the vitamin B12 uptake pathway to non-invasively probe the nutrient demand of cancer cells. The synthesis, characterization, and tumor-homing properties of a vitamin B12 PET radiotracer are described.
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Dr. Jianxun Lu, Lei Lei, Yi Huan, Yongqiang Li, Dr. Lijing Zhang, Zhufang Shen, Dr. Wenxiang Hu and Zhiqiang Feng
Article first published online: 15 APR 2014 | DOI: 10.1002/cmdc.201400009
Two birds, one stone: GK/PPARγ dual-target ligands were constructed by rational combination of pharmacophores from known GK activators and PPARγ agonists. Their ability to induce GK and PPARγ transcriptional activity were evaluated, and the putative binding modes of one of the most promising compounds were also explored by molecular docking simulations with GK and PPARγ.
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Dr. Thierry Bernardi, Stéphanie Badel, Dr. Pascal Mayer, Jérome Groelly, Dr. Pierre de Frémont, Dr. Béatrice Jacques, Dr. Pierre Braunstein, Dr. Marie-Laure Teyssot, Christelle Gaulier, Dr. Federico Cisnetti, Dr. Arnaud Gautier and Dr. Sylvain Roland
Article first published online: 11 APR 2014 | DOI: 10.1002/cmdc.201402012
Film screening: Metal-N-heterocyclic carbene (NHC) complexes of group 11 metals (Ag, Au, Cu) strongly inhibit biofilm formation by representative pathogenic bacteria at low concentrations. The highest and broadest activities are obtained with silver as the metal complexed with lipophilic NHCs. This opens new perspectives to develop alternative drugs to treat biofilm-associated pathogens.