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Poupak Dadvar Duangnapa Kovanich Gert E. Folkers Dr. Klaus Rumpel Dr. Reinout Raijmakers Dr. Albert J. R. Heck Prof. Dr. 《Chembiochem : a European journal of chemical biology》2009,10(16):2654-2662
Identifying protein “interactors” of drugs is of great importance to understand their mode of action and possible cross‐reactivity to off‐target protein binders. In this study, we profile proteins that bind to PF‐3717842, a high‐affinity phosphodiesterase‐5 (PDE5) inhibitor, by using a refined affinity pulldown approach with PF‐3717842 immobilized beads. By performing these pulldowns in rat testis tissue lysate, we strongly and specifically enriched for PDE5 and a few other PDEs. In addition to these expected affinity‐enriched proteins we also detect rodent‐specific phosphatidylethanolamine‐binding protein 2 (PEBP2), as a putative binder to the PDE5 inhibitor. By using recombinant forms of the related murine mPEBP2, mPEBP1 and human hPEBP1 (also known as Raf kinase inhibitor protein or RKIP) we confirm that they all can bind strongly to immobilized as well as soluble PF‐3717842. As the phosphatidylethanolamine‐binding proteins are involved in various important signal transduction pathways, the synthetic PDE5 inhibitor used here might form a platform to synthesize enhanced binders/inhibitors of the family of PEBP proteins. Our approach shows how chemical proteomics might be used to profile the biochemical space (interactome) of small molecule inhibitors. 相似文献
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Cover Picture: Conformational Flexibility in the Binding Surface of the Potassium Channel Blocker ShK (ChemBioChem 16/2014) 下载免费PDF全文
Inbal Sher Shih Chieh Chang Dr. Ying Li Dr. Sandeep Chhabra Prof. Arthur G. Palmer III Prof. Raymond S. Norton Dr. Jordan H. Chill 《Chembiochem : a European journal of chemical biology》2014,15(16):2317-2317
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Cover Picture: Hot‐Spot Residues in the Cytochrome P450cam–Putidaredoxin Binding Interface (ChemBioChem 1/2014) 下载免费PDF全文
Yoshitaka Hiruma Ankur Gupta Alexander Kloosterman Caroline Olijve Betül Ölmez Dr. Mathias A. S. Hass Prof. Dr. Marcellus Ubbink 《Chembiochem : a European journal of chemical biology》2014,15(1):1-1
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Sylvain Petit Yann Duroc Dr. Valéry Larue Dr. Carmela Giglione Dr. Carole Léon Dr. Coralie Soulama Dr. Alexis Denis Dr. Frédéric Dardel Prof. Thierry Meinnel Dr. Isabelle Artaud Dr. 《ChemMedChem》2009,4(2):133-133
The cover picture shows a “reverse” indole derivative in complex with Bacillus stearothermophilus peptide deformylase (PDF). This compound was selected from a structure–activity relationship study as a potent inhibitor of bacterial PDFs and shows antibacterial activity toward Bacillus subtilis as well as other pathogens such as Streptococcus pneumoniae and Staphylococcus aureus. For more details, see the Full Paper by I. Artaud et al. on p. 261 ff.
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Cover Picture: Peptidyl Succinimidyl Peptides as Taspase 1 Inhibitors (ChemBioChem 15/2014) 下载免费PDF全文
Johannes van den Boom Marija Mamić Daniele Baccelliere Dr. Susanne Zweerink Dr. Farnusch Kaschani Prof. Dr. Shirley Knauer Prof. Dr. Peter Bayer Prof. Dr. Markus Kaiser 《Chembiochem : a European journal of chemical biology》2014,15(15):2165-2165
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Cover Picture: Towards the Development of Small‐Molecule MO25 Binders as Potential Indirect SPAK/OSR1 Kinase Inhibitors (ChemBioChem 5/2017) 下载免费PDF全文
Dr. Hachemi Kadri Mubarak A. Alamri Dr. Iva H. Navratilova Dr. Luke J. Alderwick Prof. Nigel S. Simpkins Dr. Youcef Mehellou 《Chembiochem : a European journal of chemical biology》2017,18(5):424-424