Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1,-2, and-3 with altered selectivity

…, SC Yoder, G Biddlecome, RW Hungate…

文献索引：Frohn, Mike; Viswanadhan, Vellarkad; Pickrell, Alexander J.; Golden, Jennifer E.; Muller, Kristine M.; Buerli, Roland W.; Biddlecome, Gloria; Yoder, Sean C.; Rogers, Norma; Dao, Jennifer H.; Hungate, Randall; Allen, Jennifer R. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 18 p. 5023 - 5026

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被引用次数: 23

摘要

Intracellular levels of the hypoxia-inducible transcription factor (HIF) are regulated under normoxic conditions by prolyl hydroxylases (PHD1, 2, and 3). Treatment of cells with PHD inhibitors stabilizes HIF-1α, eliciting an artificial hypoxic response that includes the transcription of genes involved in erythropoiesis, angiogenesis, and glycolysis. The different in vivo roles of the three PHD isoforms are not yet known, making a PHD-selective ...