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Molecules 2015, 20(11), 20551-20568; doi:10.3390/molecules201119717

Recent Advances in Developing Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylases and Their Therapeutic Implications

1
Center for Theragnosis, Biomedical Research Institute, Korea Institute of Science and Technology, Hwarangno 14-gil 5, Seongbuk-gu, Seoul 136-791, Korea
2
Department of Biomedical Engineering, Korea University of Science and Technology (UST), KIST campus, Seoul 136-791, Korea
3
Department of Biological Chemistry, Korea University of Science and Technology (UST), KIST campus, Seoul 136-791, Korea
*
Author to whom correspondence should be addressed.
Academic Editor: Peter Willett
Received: 14 October 2015 / Revised: 10 November 2015 / Accepted: 11 November 2015 / Published: 19 November 2015
(This article belongs to the Special Issue Chemoinformatics)
View Full-Text   |   Download PDF [3316 KB, uploaded 19 November 2015]   |  

Abstract

Hypoxia-inducible factor (HIF) prolyl hydroxylases (PHDs) are members of the 2-oxoglutarate dependent non-heme iron dioxygenases. Due to their physiological roles in regulation of HIF-1α stability, many efforts have been focused on searching for selective PHD inhibitors to control HIF-1α levels for therapeutic applications. In this review, we first describe the structure of PHD2 as a molecular basis for structure-based drug design (SBDD) and various experimental methods developed for measuring PHD activity. We further discuss the current status of the development of PHD inhibitors enabled by combining SBDD approaches with high-throughput screening. Finally, we highlight the clinical implications of small molecule PHD inhibitors. View Full-Text
Keywords: prolyl hydroxylase (PHD) inhibitor; hypoxia-inducible factor (HIF); structure-based drug design (SBDD); high-throughput screening (HTS) prolyl hydroxylase (PHD) inhibitor; hypoxia-inducible factor (HIF); structure-based drug design (SBDD); high-throughput screening (HTS)
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Kim, S.Y.; Yang, E.G. Recent Advances in Developing Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylases and Their Therapeutic Implications. Molecules 2015, 20, 20551-20568.

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