Title : Discovery of oridonin as a novel agonist for BRS-3.

Pub. Date : 2022 Jun

PMID : 35405616






9 Functional Relationships(s)
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1 Discovery of oridonin as a novel agonist for BRS-3. oridonin bombesin-like receptor 3 Mus musculus
2 Recent studies have shown that BRS-3 played a vital role in glucose regulation, insulin secretion, and energy homeostasis. Glucose bombesin-like receptor 3 Mus musculus
3 To further validate the target of BRS-3, a series of in vitro and in vivo experiences were conducted, including glucose uptake, glucose transporter type 4 (GLUT4) transportation in C2C12, and oral glucose tolerance test (OGTT) in mice. Glucose bombesin-like receptor 3 Mus musculus
4 To further validate the target of BRS-3, a series of in vitro and in vivo experiences were conducted, including glucose uptake, glucose transporter type 4 (GLUT4) transportation in C2C12, and oral glucose tolerance test (OGTT) in mice. Glucose bombesin-like receptor 3 Mus musculus
5 RESULTS: We discovered and identified oridonin as a novel small molecule agonist of BRS-3, with a moderate affinity (EC50 of 2.236 x 10-7 M in calcium mobilization assay), specificity, and subtype selectivity. oridonin bombesin-like receptor 3 Mus musculus
6 Further in vitro and in vivo tests demonstrated that oridonin exerted beneficial effects in glucose homeostasis through activating BRS-3. oridonin bombesin-like receptor 3 Mus musculus
7 Further in vitro and in vivo tests demonstrated that oridonin exerted beneficial effects in glucose homeostasis through activating BRS-3. Glucose bombesin-like receptor 3 Mus musculus
8 CONCLUSIONS: Oridonin, as the discovered new ligand of BRS-3, provides a valuable tool compound to investigate BRS-3"s function, especially for target validation in type 2 diabetes and obesity. oridonin bombesin-like receptor 3 Mus musculus
9 CONCLUSIONS: Oridonin, as the discovered new ligand of BRS-3, provides a valuable tool compound to investigate BRS-3"s function, especially for target validation in type 2 diabetes and obesity. oridonin bombesin-like receptor 3 Mus musculus