ArticlePharmacology research & perspectives2019
Discovery and characterization of a small-molecule enteropeptidase inhibitor, SCO-792.
Article in Pharmacology research & perspectives, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 15 citations in OpenAlex.
- An Exploratory Randomized Trial of SCO-792, an Enteropeptidase Inhibitor, in Patients With Type 2 Diabetes and Albuminuria.Kidney international reports · 2023Article
- Cryo-EM structures reveal the activation and substrate recognition mechanism of human enteropeptidase.Nature communications · 2022Article
- Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity.Journal of medicinal chemistry · 2022Article
- The Global Status and Trends of Enteropeptidase: A Bibliometric Study.Frontiers in medicine · 2022Article
- Enteropeptidase inhibitor SCO-792 effectively prevents kidney function decline and fibrosis in a rat model of chronic kidney disease.Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association · 2021Article
- Review
- Enteropeptidase inhibition improves kidney function in a rat model of diabetic kidney disease.Diabetes, obesity & metabolism · 2021Article
- Discovery and characterization of a small-molecule enteropeptidase inhibitor, SCO-792.Pharmacology research & perspectives · 2019Article
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Authors and funding
13 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Enteropeptidase, localized into the duodenum brush border, is a key enzyme catalyzing the conversion of pancreatic trypsinogen proenzyme to active trypsin, thereby regulating protein digestion and energy homeostasis. We report the discovery and pharmacological profiles of SCO-792, a novel inhibitor of enteropeptidase. A screen employing fluorescence resonance energy transfer was performed to identify enteropeptidase inhibitors. Inhibitory profiles were determined by in vitro assays. To evaluate the in vivo inhibitory effect on protein digestion, an oral protein challenge test was performed in rats. Our screen identified a series of enteropeptidase inhibitors, and compound optimization resulted in identification of SCO-792, which inhibited enteropeptidase activity in vitro, with IC
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