Kim, So Yeon Yang, Eun Gyeong 2024-01-20T06:00:40Z 2024-01-20T06:00:40Z 2021-09-04 2015-11 1420-3049 https://pubs.kist.re.kr/handle/201004/124852 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. English MDPI FOCAL CEREBRAL-ISCHEMIA VHL TUMOR-SUPPRESSOR FACTOR-I OXYGEN SENSORS 4-HYDROXYLASE INHIBITORS DOMAIN PROTEIN-2 NORMOXIC CELLS HIF PATHWAY HIF-1-ALPHA ASSAY Recent Advances in Developing Inhibitors for Hypoxia-Inducible Factor Prolyl Hydroxylases and Their Therapeutic Implications Article 10.3390/molecules201119717 1 MOLECULES, v.20, no.11, pp.20551 - 20568 MOLECULES 20 11 20551 20568 scie scopus 000365925200022 2-s2.0-84949987814 Biochemistry & Molecular Biology Chemistry, Multidisciplinary Biochemistry & Molecular Biology Chemistry Review FOCAL CEREBRAL-ISCHEMIA VHL TUMOR-SUPPRESSOR FACTOR-I OXYGEN SENSORS 4-HYDROXYLASE INHIBITORS DOMAIN PROTEIN-2 NORMOXIC CELLS HIF PATHWAY HIF-1-ALPHA ASSAY prolyl hydroxylase (PHD) inhibitor hypoxia-inducible factor (HIF) structure-based drug design (SBDD) high-throughput screening (HTS)