Portales-Castillo Ignacio, Höppner Jakob, Jüppner Harald, Gardella Thomas J
Department of Medicine, Division of Nephrology, Washington University in St. Louis, St. Louis, MO, United States.
Endocrine Unit, Massachusetts General Hospital, and Harvard Medical School, Boston, MA, United States.
Front Endocrinol (Lausanne). 2025 Aug 19;16:1641292. doi: 10.3389/fendo.2025.1641292. eCollection 2025.
The parathyroid hormone receptor type 1 (PTH1R) is a G protein-coupled receptor that mediates the actions of parathyroid hormone (PTH) in the regulation of blood calcium levels, as well as PTH-related protein (PTHrP) in the regulation of skeletal development. Severe loss-of-function homozygous mutations in PTH1R are incompatible with life as in Blomstrand's lethal chondrodysplasia, characterized by accelerated growth plate ossification. More recently, homozygous mutations located in the transmembrane helices, extracellular domains and C-tail of the PTH1R were identified in patients with milder conditions characterized by variable degrees of skeletal and mineral abnormalities. These include delayed ossification in Eiken syndrome, hypocalcemia in a pseudohypoparathyroidism-like disorder, and non-syndromic primary failure of tooth eruption; which is usually caused by heterozygous PTH1R mutations. Recent detailed pharmacologic characterization of these PTH1R mutants has revealed new insights into how even subtle perturbations in PTH1R function can result in disease.
甲状旁腺激素1型受体(PTH1R)是一种G蛋白偶联受体,它介导甲状旁腺激素(PTH)在调节血钙水平中的作用,以及甲状旁腺激素相关蛋白(PTHrP)在调节骨骼发育中的作用。PTH1R中严重的功能丧失性纯合突变与生命不相容,如布洛姆斯特兰德致死性软骨发育不良,其特征是生长板骨化加速。最近,在症状较轻的患者中发现了位于PTH1R跨膜螺旋、细胞外结构域和C末端的纯合突变,这些患者具有不同程度的骨骼和矿物质异常。这些异常包括艾肯综合征中的骨化延迟、类似假性甲状旁腺功能减退症的疾病中的低钙血症,以及非综合征性原发性出牙失败;这些通常由杂合性PTH1R突变引起。最近对这些PTH1R突变体的详细药理学特征分析揭示了新的见解,即即使PTH1R功能的细微扰动也会导致疾病。