Water-Based Ligand Screening for Paramagnetic Metalloproteins

The relaxation rate of water proton nuclei can be used to screen ligands (L; see picture) directed to the metal binding site in paramagnetic metalloproteins by NMR spectroscopy. The very high concentration of water protons provides an enormous sensitivity and permits the use of unprecedentedly low a...

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Veröffentlicht in:	Angewandte Chemie (International ed.) 2008-06, Vol.47 (24), p.4533-4537
Hauptverfasser:	Bertini, Ivano, Fragai, Marco, Luchinat, Claudio, Talluri, Eleonora
Format:	Artikel
Sprache:	eng
Schlagworte:	drug design Drug Evaluation, Preclinical - methods Ligands Magnetic Resonance Spectroscopy - methods Magnetics metalloenzymes metalloproteins Metalloproteins - chemistry NMR spectroscopy Nuclear Proteins - antagonists & inhibitors Nuclear Proteins - chemistry Phosphoprotein Phosphatases - antagonists & inhibitors Phosphoprotein Phosphatases - chemistry proton relaxation Water - chemistry
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Beschreibung
Zusammenfassung:	The relaxation rate of water proton nuclei can be used to screen ligands (L; see picture) directed to the metal binding site in paramagnetic metalloproteins by NMR spectroscopy. The very high concentration of water protons provides an enormous sensitivity and permits the use of unprecedentedly low amounts of protein.
ISSN:	1433-7851 1521-3773
DOI:	10.1002/anie.200800327