- parathyroid hormone 1 receptor
- Available assay modes
- Agonist, Inverse agonist, Antagonist, PAM, NAM
- à la carte, Oncology, Hematology, Endocrinology/Metabolism, Ophthalmology, Respiratory, Musculoskeletal, Urology/Reproduction, Human non-orphan GPCRs
Parathyroid hormone receptorsThe 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 . Another structure of a PTH-(1-34) analog bound to a thermostabilized inactive PTH1 receptor has been obtained with X-ray crytallography .
- Zhao LH, Ma S, Sutkeviciute I, et al. Structure and dynamics of the active human parathyroid hormone receptor-1. Science 2019;364:148-153.
- 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
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