Different Modes of Inhibitor Binding to Prolyl Hydroxylase by Combined Use of X-ray Crystallography and NMR Spectroscopy of Paramagnetic Complexes

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• 作者：Leszek Poppe ; Christopher M. Tegley ; Vivian Li ; Jeffrey Lewis ; James Zondlo ; Evelyn Yang ; Robert JM Kurzeja ; Rashid Syed
• 刊名：Journal of the American Chemical Society
• 出版年：2009
• 出版时间：November 25, 2009
• 年：2009
• 卷：131
• 期：46
• 页码：16654-16655
• 全文大小：114K
• 年卷期：v.131,no.46(November 25, 2009)
• ISSN：1520-5126

文摘

In aqueous solution, azaquinolone inhibitors bind to prolyl 4-hydroxylase in two different orientations, as first detected by ¹⁹F spectroscopy. This contrasts with the crystallographic structure where only one orientation has been determined. Dissection of the metal binding properties of the enzyme allowed structures of both complexes to be obtained in solution from ¹⁹F and ¹³C dipolar shifts in a labeled ligand.