2020
DOI: 10.3390/ijms21186613
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Develop a High-Throughput Screening Method to Identify C-P4H1 (Collagen Prolyl 4-Hydroxylase 1) Inhibitors from FDA-Approved Chemicals

Abstract: Collagen prolyl 4-hydroxylase 1 (C-P4H1) is an α-ketoglutarate (α-KG)-dependent dioxygenase that catalyzes 4-hydroxylation of proline on collagen. C-P4H1-induced prolyl hydroxylation is required for proper collagen deposition and cancer metastasis. Therefore, targeting C-P4H1 is considered a potential therapeutic strategy for collagen-related cancer progression and metastasis. However, no C-P4H1 inhibitors are available for clinical testing, and the high content assay is currently not available for C-P4H1 inhi… Show more

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Cited by 4 publications
(2 citation statements)
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“…Subsequently, a number of prolyl hydroxylase inhibitors have been studied in vitro but issues related to toxicity, side effects, or specificity have limited their translation to the clinic. Efforts continue to identify new categories of inhibitors ( 50 , 51 ).…”
Section: Ptms: Roles In the Structure And Function Of Ecm Proteinsmentioning
confidence: 99%
“…Subsequently, a number of prolyl hydroxylase inhibitors have been studied in vitro but issues related to toxicity, side effects, or specificity have limited their translation to the clinic. Efforts continue to identify new categories of inhibitors ( 50 , 51 ).…”
Section: Ptms: Roles In the Structure And Function Of Ecm Proteinsmentioning
confidence: 99%
“…Targeting collagen prolyl 4-hydroxylase 1 (C-P4H1) is considered a potential therapeutic strategy for collagen-related cancer progression and metastasis. Shike Wang et al [8] developed a high-throughput screening assay for C-P4H1 inhibitor screening by quantifying succinate, a byproduct of C-P4H-catalyzed hydroxylation. They performed highthroughput screening with the FDA-approved drug library and identified several new C-P4H1 inhibitors, including Silodosin and Ticlopidine.…”
mentioning
confidence: 99%