Concepedia

Discovery and Preclinical Characterization of GSK1278863 (Daprodustat), a Small Molecule Hypoxia Inducible Factor–Prolyl Hydroxylase Inhibitor for Anemia

Jennifer L. Ariazi, Kevin J. Duffy, David F. Adams, Duke M. Fitch, Lusong Luo, Melissa B. Pappalardi, Mangatt P. Biju, Erin Hugger DiFilippo, Tony Shaw, Ken Wiggall,

Journal of Pharmacology and Experimental Therapeutics · 2017 · 91 citations · 55 references

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References

55

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

Yung-Chi Cheng, William H. Prusoff · Biochemical Pharmacology · 1973 · 12.9K citations

, , +14

Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension.

G L Wang, Bing‐Hua Jiang, E A Rue et al. · Proceedings of the National Academy of Sciences · 1995 · 6.2K citations

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Targeting of HIF-α to the von Hippel-Lindau Ubiquitylation Complex by O <sub>2</sub> -Regulated Prolyl Hydroxylation

Panu Jaakkola, David R. Mole, Ya‐Min Tian et al. · Science · 2001 · 5.5K citations

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The tumour suppressor protein VHL targets hypoxia-inducible factors for oxygen-dependent proteolysis

Patrick H. Maxwell, Michael S. Wiesener, Gin-Wen Chang et al. · Nature · 1999 · 5.2K citations

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HIFα Targeted for VHL-Mediated Destruction by Proline Hydroxylation: Implications for O <sub>2</sub> Sensing

Mircea Ivan, Keiichi Kondo, Haifeng Yang et al. · Science · 2001 · 4.7K citations · Full text

, , +16