Recent Advances in Developing Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylases and Their Therapeutic ImplicationsReport as inadecuate




Recent Advances in Developing Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylases and Their Therapeutic Implications - Download this document for free, or read online. Document in PDF available to download.

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

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





Author: So Yeon Kim 1,2 and Eun Gyeong Yang 1,3,*

Source: http://mdpi.com/



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