Human PTH1R

Figure. Concentration-dependent activation of PTH1R by PTH

Reporter cells were transfected with either the expression plasmid for human parathyroid hormone 1 receptor (PTH1R) or the mock plasmid and treated with various concentrations of PTH. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 2.2 nM.

Nomenclature
parathyroid hormone 1 receptor
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
Panels
à la carte, Oncology, Hematology, Endocrinology/Metabolism, Ophthalmology, Respiratory, Musculoskeletal, Urology/Reproduction, Human non-orphan GPCRs

Parathyroid hormone receptors

The parathyroid hormone receptors are class B G protein-coupled receptors. The parathyroid hormone (PTH)/parathyroid hormone-related peptide (PTHrP) receptor (PTH1 receptor) is activated by precursor-derived peptides: PTH (84 amino acids), and PTHrP (141 amino-acids) and related peptides (PTH-(1-34), PTHrP-(1-36)). The parathyroid hormone 2 receptor (PTH2 receptor) is activated by the precursor-derived peptide TIP39 (39 amino acids). [125I]PTH may be used to label both PTH1 and PTH2 receptors. The structure of a long-active PTH analogue (LA-PTH, an hybrid of PTH-(1-13) and PTHrP-(14-36)) bound to the PTH1 receptor-Gs complex has been resolved by cryo-electron microscopy [1]. Another structure of a PTH-(1-34) analog bound to a thermostabilized inactive PTH1 receptor has been obtained with X-ray crytallography [2].

References

  1. Zhao LH, Ma S, Sutkeviciute I, et al. Structure and dynamics of the active human parathyroid hormone receptor-1. Science 2019;364:148-153.
  2. Ehrenmann J, Schöppe J, Klenk C, et al. High-resolution crystal structure of parathyroid hormone 1 receptor in complex with a peptide agonist. Nat Struct Mol Biol 2018;25:1086-1092.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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