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Reports from N. Lancelot and Colleagues Advance Knowledge in Pharmaceutical and Biomedical Analysis (Applications of NMR screening techniques to the...

July 1, 2014



Reports from N. Lancelot and Colleagues Advance Knowledge in Pharmaceutical and Biomedical Analysis (Applications of NMR screening techniques to the pharmaceutical target Checkpoint kinase 1)

By a News Reporter-Staff News Editor at Life Science Weekly -- Investigators publish new report on Biotechnology. According to news reporting out of Croissy sur Seine, France, by NewsRx editors, research stated, "Ligand screening techniques based on NMR spectroscopy are not as sensitive as other commonly used methods like fluorescence, radiolabeling and surface plasmon resonance. However, using modern NMR instrumentation, they can achieve reliable screening under near physiological condition using as little as 4.6 nmol of receptor and 100 nmol of ligand."

Our news journalists obtained a quote from the research, "Additionally, these NMR methods can also provide valuable and specific information on the ligand under investigation such as the dissociation constant KID, the binding epitope and most importantly some structural information on the actual conformation in the bound state. In this manuscript, we describe the use of NMR based screening techniques ('Saturation Transfer Difference' (STD) and 'Water Ligand Observed via Gradient SpectroscopY' (WaterLOGSY)) to detect small therapeutic molecules that interact with the DNA damage checkpoint enzyme Checkpoint kinase 1 (Chkl). After the identification of the most potent ligand, we used specific NMR experiments to perform the epitope mapping of this ligand ('Group epitope mapping-STD' (GEM-STD), 'Difference of Inversion REcovery rate with and without Target IrradiatiON' (DIRECTION)) and to characterize its bound conformation ('Transferred-Nuclear Overhauser Effect SpectroscopY' (tr-NOESY), 'Transferred-Rotating frame Overhauser Effect SpectroscopY' (tr-ROESY)). Finally, we used molecular docking procedures to position the ligand within the active site of Chkl."

According to the news editors, the research concluded: "On the experimental level, a comparison between NMR studies performed in a 90%H2O/10%D2O buffer and a 100% D2O buffer is also presented and discussed."

For more information on this research see: Applications of NMR screening techniques to the pharmaceutical target Checkpoint kinase 1. Journal of Pharmaceutical and Biomedical Analysis, 2014;93():125-135. Journal of Pharmaceutical and Biomedical Analysis can be contacted at: Elsevier Science Bv, PO Box 211, 1000 Ae Amsterdam, Netherlands. (Elsevier - www.elsevier.com; Journal of Pharmaceutical and Biomedical Analysis - www.elsevier.com/wps/product/cws_home/525434)

Our news journalists report that additional information may be obtained by contacting N. Lancelot, Inst Rech Servier, Chim Partenariats & Modelisat Mol, F-78290 Croissy Sur Seine, France. Additional authors for this research include M. Piotto, I. Theret, B. Lesur and P. Hennig (see also Biotechnology).

Keywords for this news article include: Biotechnology, France, Europe, Kinase, Croissy sur Seine, Enzymes and Coenzymes

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC


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Source: Life Science Weekly


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