• Purity

  >95%, by SDS-PAGE visualized with Silver Staining and quantitative densitometry by Coomassie® Blue Staining

• Endotoxin Level

  <0.10 EU per 1 μg of the protein by the LAL method.  

• Activity

  Measured by its binding ability in a functional ELISA. When Recombinant Human PTH1R/PTHR1 is used at 2 μg/mL, the concentration of biotinylated human PTHrP that produces 50% of the optimal binding response is found to be approximately 0.03 ‑ 0.12 μg/mL.

• Source

  Chinese Hamster Ovary cell line, CHO-derived Tyr23-Met189, with a C-terminal 6-His tag

• Accession #

• N-terminal Sequence    
  Analysis

  Tyr23

• Predicted Molecular Mass

  20.0 kDa

• SDS-PAGE

  25-40 kDa, reducing conditons

Background: PTH1R/PTHR1

PTH1R (parathyroid receptor-1, also called PTHR1) is an 85-95 kDa member of the G-protein coupled receptor family 2 that is a critical receptor regulating Ca⁺⁺ homeostasis (1-5). The human PTH1R cDNA encodes 593 amino acids (aa) including a 26 aa signal sequence and a long extracellular domain (aa 27-189) that contains the PTH (parathyroid hormone) and PTHrP (PTH-related protein) docking site (aa 173-189), followed by seven transmembrane domains within the C-terminal 404 aa (2-4). Within the N-terminal ECD, human PTH1R shares 87%, 88%, 96%, 94% and 93% aa identity with mouse, rat, canine, bovine and porcine PTH1R, respectively. PTH of other mammals will bind and stimulate human PTH1R, although with differing affinities (2). PTH1R is mainly expressed in bone and kidney, but is also present on hepatocytes, smooth muscle cells, and in other tissues where PTH and PTHrP are found (1-3, 5, 6). Through PTH1R on osteoblasts, PTH promotes differentiation of osteoclasts, which in turn promote release of Ca⁺⁺ from bone (1, 5). PTH1R on osteocytes, however, allows PTH to promote bone formation (7). In renal epithelium, it promotes conversion of Vitamin D to its active form, lowers Ca⁺⁺ excretion and increases phosphate excretion (1, 5). Following PTH binding, PTH1R undergoes a conformation change which activates cAMP, IP3, PKC and Ca⁺⁺ signaling pathways (1, 8). PTH1R is then phosphorylated and downregulated by internalization (9). Dwarfism in Jansen‑type metaphyseal chondrodysplasia is associated with PTH1R gain of function, while in Blomstrand chondrodysplasia, PTH1R function is lost (10, 11). Impaired PTH1R function may be a factor in developmental endochondromas in Ollier disease (12). Polymorphisms may also be associated with variation in bone mineral density (13).

• References:

1. Potts, J.T. (2005) J. Endocrinol. 187:311.

2. Schipani, E. et al. (1993) Endocrinology 132:2157.

3. Zhou, A.T. et al. (1997) Proc. Natl. Acad. Sci. USA 94:3644.

4. Pellegrini, M. et al. (1998) Biochemistry 37:12737.

5. Lupp, A. et al. (2010) Eur. J. Endocrinol. 162:979.

6. Watson, P.H. et al. (2000) J. Bone Miner. Res. 15:1033.

7. O’Brien, C.A. et al. (2008) PLoS ONE 3:e2942.

8. Thomas, B.E. et al. (2008) Mol. Endocrinol. 22:1154.

9. Bounoutas, G.S. et al. (2006) Endocrinology 147:4674.

10. Schipani, E. et al. (1995) Science 268:98.

11. Wysolmerski, J.J. (2001) J. Clin. Endocrinol. Metab. 86:1788.

12. Couvineau, A. et al. (2008) Hum. Mol. Genet. 17:2766.

13. Vilarino-Guell, C. et al. (2007) Calcif Tissue Int. 81:270.

• Long Name:

  Parathyroid Hormone Receptor 1

• Entrez Gene IDs:

  5745 (Human); 19228 (Mouse); 56813 (Rat)

• Alternate Names:

  MGC138426; parathyroid hormone 1 receptorMGC138452; parathyroid hormone/parathyroid hormone-related peptide receptor; parathyroid hormone/parathyroid hormone-related protein receptor; PFE; PTH/PTHr receptor; PTH/PTHrP type I receptor; PTH1 receptor; PTH1R; PTHR; PTHR1; PTHRPTHR1parathyroid hormone receptor 1; seven transmembrane helix receptor