PTHR1 in Bone

Carole Le Henaff, Nicola C. Partridge

    Research output: Chapter in Book/Report/Conference proceedingChapter

    Abstract

    Parathyroid hormone receptor type 1 or PTHR1 is a member of the G-protein coupled receptor family. It is activated by specific endogenous ligands such as parathyroid hormone (PTH) and parathyroid hormone related protein (PTHrP). Depending on the ligand, the receptor will differentially activate pathways in bone cells. Interestingly, PTH through PTHR1 can have anabolic or catabolic actions through bone cells of the osteoblastic lineage. When PTH (1-34) is given in a pulsatile or intermittent daily fashion, it causes an increase in bone accrual. Following these observations, PTHR1 was targeted for potential osteoanabolic strategies for treating osteoporosis, with PTH (1-34) approved for this use in 2002. In 2017, fifteen years after teriparatide’s approval (PTH (1-34)), the FDA approved TymlosTM (or abaloparatide, more similar to PTHrP, 1-34, than PTH, 1-34) as a second peptide osteoanabolic treatment that acts through PTHR1. However, the effects of PTH (1-34) or its analogs as osteoanabolic treatments are complex and still not completely elucidated. PTHR1 and its pathways have also been studied as a potential target or diagnostic tool in cancers.

    Original languageEnglish (US)
    Title of host publicationGPCRs as Therapeutic Targets
    PublisherWiley
    Pages732-766
    Number of pages35
    Volume2
    ISBN (Electronic)9781119564782
    ISBN (Print)9781119564744
    DOIs
    StatePublished - Jan 1 2021

    Keywords

    • PTH
    • PTHR1
    • PTHrP
    • abaloparatide
    • cancer
    • osteoporosis

    ASJC Scopus subject areas

    • General Chemistry
    • General Pharmacology, Toxicology and Pharmaceutics
    • General Biochemistry, Genetics and Molecular Biology
    • General Medicine

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