β-Arrestin-Dependent Parathyroid Hormone-Stimulated Extracellular Signal-Regulated Kinase Activation and Parathyroid Hormone Type 1 Receptor Internalization [PDF]
Endocrinology, 2007 PTH regulates renal calcium homeostasis by actions on the distal nephron. PTH-induced calcium transport in mouse distal convoluted tubule (DCT) cells requires activation of ERK1/2. ERK activation by β-adrenergic receptors occurs in a biphasic manner and involves receptor internalization.
W Bruce, Sneddon, Peter A, Friedman
openaire +2 more sources
Actions of the Small Molecule Ligands SW106 and AH-3960 on the Type-1 Parathyroid Hormone Receptor [PDF]
Molecular Endocrinology, 2015 AbstractThe parathyroid hormone receptor-1 (PTHR1) plays critical roles in regulating blood calcium levels and bone metabolism and is thus of interest for small-molecule ligand development. Of the few small-molecule ligands reported for the PTHR1, most are of low affinity, and none has a well-defined mechanism of action. Here, we show that SW106 and AH-
Percy H, Carter +5 more
openaire +2 more sources
Clinical Unmet Needs in Hypoparathyroidism and Current Pipeline Agents
Endocrinology Research and PracticeHypoparathyroidism is a disease characterized by inadequate or absent parathyroid hormone (PTH) levels. It manifests with hypocalcemia, hyperphosphatemia, and elevated urinary fractional excretion of calcium.
Ecesu Çetin +2 more
doaj +3 more sources
Selective Ligand-induced Stabilization of Active and Desensitized Parathyroid Hormone Type 1 Receptor Conformations [PDF]
Journal of Biological Chemistry, 2002 For many G protein-coupled receptors, agonist-induced activation is followed by desensitization, internalization, and resensitization. In most cases, these processes are dependent upon interaction of agonist-occupied receptor with cytoplasmic beta-arrestins.
Alessandro, Bisello +5 more
openaire +2 more sources
Hormonal changes during aging and their effects on quality of life [PDF]
Exploration of Endocrine and Metabolic DiseasesHormonal dysregulation plays a central role in aging, exerting a profound, multidimensional impact on quality of life. This narrative review examines the impact of hormonal changes in understanding how age-dependent alterations in key hormonal axes ...
Carter Coggins +3 more
doaj +1 more source
Abnormal Renovascular Parathyroid Hormone-1 Receptor in Hypertension: Primary Defect or Secondary to Angiotensin II Type 1 Receptor Activation? [PDF]
Endocrinology, 2006 We previously reported that PTHrP-induced renal vasodilation is impaired in mature spontaneously hypertensive rats (SHR) through down-regulation of the type 1 PTH/PTHrP receptor (PTH1R), a feature that contributes to the high renal vascular resistance in SHR.
Sandra, Welsch +6 more
openaire +2 more sources
BMC Musculoskeletal Disorders, 2020 Background Fractures in older men are not uncommon and need to be healed as soon as possible to avoid related complications. Anti-osteoporotic drugs targeting Wnt/β-catenin and PTH (parathyroid hormone) to promote fracture healing have become an ...
Daocheng Liu +8 more
doaj +1 more source
Altered Signaling and Desensitization Responses in PTH1R Mutants Associated with Eiken Syndrome
Communications Biology, 2023 The parathyroid hormone receptor type 1 (PTH1R) is a G protein-coupled receptor that plays key roles in regulating calcium homeostasis and skeletal development via binding the ligands, PTH and PTH-related protein (PTHrP), respectively.
Ignacio Portales-Castillo +8 more
doaj +1 more source
Modulation of β-catenin signaling by glucagon receptor activation. [PDF]
PLoS ONE, 2012 The glucagon receptor (GCGR) is a member of the class B G protein-coupled receptor family. Activation of GCGR by glucagon leads to increased glucose production by the liver.
Jiyuan Ke +8 more
doaj +1 more source
Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator
Cells, 2022 The parathyroid hormone type 1 receptor (PTH1R) acts as a canonical class B G protein-coupled receptor, regulating crucial functions including calcium homeostasis and bone formation.
Mengrong Li +5 more
doaj +1 more source