Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion

Inhibition of the hypoxia-inducible factor (HIF) prolyl hydroxylases (PHD or EGLN enzymes) is of interest for the treatment of anemia and ischemia-related diseases. Most PHD inhibitors work by binding to the single ferrous ion and competing with 2-oxoglutarate (2OG) co-substrate for binding at the P...

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Veröffentlicht in:	Organic & biomolecular chemistry 2013-02, Vol.11 (5), p.732-745
Hauptverfasser:	Yeoh, Kar Kheng, Chan, Mun Chiang, Thalhammer, Armin, Demetriades, Marina, Chowdhury, Rasheduzzaman, Tian, Ya-Min, Stolze, Ineke, McNeill, Luke A, Lee, Myung Kyu, Woon, Esther C Y, Mackeen, Mukram M, Kawamura, Akane, Ratcliffe, Peter J, Mecinović, Jasmin, Schofield, Christopher J
Format:	Artikel
Sprache:	eng
Schlagworte:	Catalytic Domain Cell Line, Tumor Humans Hydrazines - chemistry Hydrazines - pharmacology Hypoxia-Inducible Factor-Proline Dioxygenases Iron - metabolism Molecular Docking Simulation Procollagen-Proline Dioxygenase - antagonists & inhibitors Procollagen-Proline Dioxygenase - chemistry Procollagen-Proline Dioxygenase - metabolism Protein Binding - drug effects Spectrometry, Mass, Electrospray Ionization
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