Differing pharmacological activities of thiazolidinone analogs at the FSH receptor.
作者： Brian J. Arey , Stephen D. Yanofsky , M. Claudia Pérez , Christopher P. Holmes , Jay Wrobel
DOI: 10.1016/J.BBRC.2008.01.119
关键词:
摘要: The follicle-stimulating hormone is critical to reproductive success and an important target for development of novel therapies. We have recently reported the thiazolidinone positive allosteric modulators receptor. Here, we demonstrate that discrete modifications in chemical structure agonists produced compounds with different pharmacological properties. Positive activated adenylate cyclase signaling (Gs). Using ADP-ribosylation assay found both differing glycosylated variants human FSH (hFSH) selected FSHR induce activation Gi pathway. Additionally, observed some analogs this class could activate pathways. These data suggest activity may be due ability these association either Gs or pathways analog-specific manner.
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