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 language | English (US) |
|---|---|
| Title of host publication | GPCRs as Therapeutic Targets |
| Publisher | Wiley |
| Pages | 732-766 |
| Number of pages | 35 |
| Volume | 2 |
| ISBN (Electronic) | 9781119564782 |
| ISBN (Print) | 9781119564744 |
| DOIs | |
| State | Published - Jan 1 2021 |
Keywords
- PTH
- PTHR1
- PTHrP
- abaloparatide
- cancer
- osteoporosis
ASJC Scopus subject areas
- Medicine(all)
- Pharmacology, Toxicology and Pharmaceutics(all)
- Biochemistry, Genetics and Molecular Biology(all)
- Chemistry(all)