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Altered signaling at the PTH receptor via modified agonist contacts with the extracellular domain provides a path to prolonged agonism in vivo

The parathyroid hormone type 1 receptor (PTHR1), a Class B GPCR, is activated by long polypeptides, including drugs for osteoporosis and hypoparathyroidism. The PTHR1 engages peptide agonists via a two-step mechanism. Initial contact involves the extracellular domain (ECD), which has been thought to...

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Detalles Bibliográficos
Autores principales: Liu, Shi, Yu, Zhen, Daley, Eileen J., Bingman, Craig A., Bruchs, Austin T., Gardella, Thomas J., Gellman, Samuel H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: National Academy of Sciences 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9860328/
https://www.ncbi.nlm.nih.gov/pubmed/36409914
http://dx.doi.org/10.1073/pnas.2212736119