Interestingly, molecular dynamics simulations reveal that antagonism is achieved through disruption of allosteric paths of communication unique to LRH-1. Our work therefore characterizes a highly efficacious small molecule LRH-1 antagonist and provides mechanistic insight into how signaling for this receptor...
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...
The back cover picture shows superimposed models for two successive events in liver receptor homolog-1 (LRH-1) blockade. 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...
The study was performed in order to try to provoke the gonadotropin wave and ovulation in Chalcarburnus chacoides using GnRH analogue, pituitary extract and dopamine antagonist. Different doses and injection protocols were applied using a combination of LRH-Aa, metoclopramide and carp pituitary ...
Prior to the onset of the spawning season female rainbow trout were injected intraperitoneally (IP) with LRH-A ([des Gly 10 D-Ala 6] LHRH ethylamide) alone at a dose of 1 渭g/kg body weight or in combination with pimozide (PIM, 10 mg/kg body weight), a dopamine antagonist, given ...
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...