In the apo-receptor, the binding site is capped with helix 12 (cream), but antagonist (green) binding fills the entrance and displaces H-12 (orange). Two side chains on the apo-protein H-12 are responsible for the steric clash. For more details, see the Communication by Simak Ali,...
These studies provide a rationale for pursuing enantiomerically pure RJW100 derivatives: they establish RR-RJW100 as the stronger LRH-1 agonist and identify a potential for optimizing the SS-RJW100 scaffold for antagonist design.doi:10.1038/s41598-020-79251-9Suzanne G. Mays...
Interleukin-1 receptor antagonist induction as an additional mechanism for liver receptor homolog-1 to negatively regulate the hepatic acute phase response J. Biol. Chem., 282 (2007), pp. 4393-4399 View PDFView articleView in ScopusGoogle Scholar [114] N. Venteclef, T. Jakobsson, A. Ehrlund...
Our work therefore characterizes a highly efficacious small molecule LRH-1 antagonist and provides mechanistic insight into how signaling for this receptor can be effectively disrupted without large structural rearrangements.doi:10.1096/fasebj.2022.36.S1.R4855Michael L. Cato...
Results Stimulation of D_1-like receptor inhibited the IGF-1 receptor expression,which was blocked by D_1-like receptor antagonist. 方法本试验以A10细胞为研究对象,免疫印迹观察刺激D_1类受体对IGF-1受体表达的影响,并初步探讨D_1类受体对IGF-1受体影响的机制。 更多例句>> 补充...