期刊
MOLECULES
卷 20, 期 11, 页码 20551-20568出版社
MDPI
DOI: 10.3390/molecules201119717
关键词
prolyl hydroxylase (PHD) inhibitor; hypoxia-inducible factor (HIF); structure-based drug design (SBDD); high-throughput screening (HTS)
资金
- Korean Ministry of Science, ICT and Future Planning
- KIST
- Ministry of Science, ICT & Future Planning, Republic of Korea [2E25270] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
- National Research Foundation of Korea [2012M3A9B9036679] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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-1 stability, many efforts have been focused on searching for selective PHD inhibitors to control HIF-1 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.
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