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... The class B G protein-coupled receptor (GPCR) calcitonin receptor (CTR) is a drug target for osteoporosis and diabetes. N-glycosylation of asparagine 130 in its extracellular domain (ECD) enhances calcitonin hormone affinity with the proximal GlcNAc residue mediating this effect through an unknown mechanism. Here, we present two crystal structures of salmon calcitonin-bound, GlcNAc-bearing CTR ECD ...
... The high level of bone metabolism associated with osteopenia and multifocal skeletal fracture remains a challenging clinical problem in osteoporosis patients. Salmon calcitonin (sCT), as a peptide medicine, is able to inhibit osteoclast activity and stimulate osteoblast growth. However, calcitonin receptors (CTRs) are widely distributed in vivo, limiting the specificity and therapeutic effects. He ...
... Variations in the mRNA expression of hepatic and muscle genes that are related to calcium signaling were analyzed by real-time qPCR in farmed Atlantic salmon (Salmo salar L. 1758) to determine changes in expression between parr and smolt stages. These organs were selected due to their close relationship with calcium signaling and metabolism (e.g., glycolysis, oxidative phosphorylation, muscle cont ...
... The calcitonin receptor (CTR) is a class B G protein-coupled receptor that is activated by the peptide hormones calcitonin and amylin. Calcitonin regulates bone remodeling through CTR, whereas amylin regulates blood glucose and food intake by activating CTR in complex with receptor activity-modifying proteins (RAMPs). These receptors are targeted clinically for the treatment of osteoporosis and di ...
alpha-melanocyte-stimulating hormone; anesthesia; body weight; bone resorption; calcitonin; calcitonin receptors; calcium; gene expression; goldfish; hormone secretion; messenger RNA; metabolism
Abstract:
... The effects of α-melanocyte-stimulating hormone (α-MSH) on calcium metabolism were examined with goldfish. The scales on the left side of goldfish bodies were removed to allow the regeneration of scales under anesthesia. Thereafter, the influences of α-MSH injection (low dose: 0.1 μg/g body weight; high dose: 1 μg/g body weight) on plasma calcitonin (calcium-regulating hormone) and the calcium con ...
... Receptor activity-modifying protein 2 (RAMP2) enables the calcitonin receptor-like receptor (CLR, a family B GPCR) to form the type 1 adrenomedullin receptor (AM1 receptor). Here, we investigated the effects of the five non-visual GPCR kinases (GRKs 2 through 6) on the cell surface expression of the human (h)AM1 receptor by cotransfecting each of these GRKs into HEK-293 cells that stably expressed ...
Silvia R. Terra; João Carlos R. Cardoso; Rute C. Félix; Leo Anderson M. Martins; Diogo Onofre G. Souza; Fatima C.R. Guma; Adelino Vicente M. Canário; Vanessa Schein
... Stanniocalcin 1 (STC1) and calcitonin gene-related peptide (CGRP) are involved in bone formation/remodeling. Here we investigate the effects of STC1 on functional heterodimer complex CALCRL/RAMP1, expression and activity during osteoblastogenesis. STC1 did not modify CALCRL and ramp1 gene expression during osteoblastogenesis when compared to controls. However, plasma membrane spatial distribution ...
... In anautogenous mosquitoes such as Aedes aegypti females the calcitonin-like diuretic hormone 31 (DH31) stimulates natriuretic fluid excretion from the Malpighian tubules (MTs) after a blood meal. We previously cloned and functionally characterized AedaeGPCRcal1 from A. aegypti, the ortholog of the Drosophila melanogaster DH31 receptor and immunolocalized it in the MTs. However, localization of th ...
... Calcitonin receptor-immunoreactivity (CTR-ir) was found in enteric neurons of the mouse gastrointestinal tract from embryonic day 13.5 (E13.5) to post-natal day 28 (P28). CTR-ir occurred in cell bodies in ganglia of the myenteric plexus extending from the esophagus to the colon and in nerve cells of the submucosal ganglia of the small and large intestines. CTR-ir was also found in vagal nerve trun ...
... Human disc degeneration initiated by aging in the central nucleus pulposus (hNP) is an irreversible process and the recovery has become seriously emerging. In this study, the related mechanisms of calcitonin on the regeneration of hNP and the effects of calcitonin on the age-related alterations were examined. The harvested hNP population was designated as YhNP (from young donor, age <50) and OhNP ...
... In cartilaginous fish, two cDNAs encoding calcitonin-family receptors were isolated for the first time from the stingray brain. The open reading frame of one receptor cDNA coded a 525-amino acid protein. The amino acid identity of this receptor to human calcitonin-receptor-like receptor (CRLR) is 64.5%, frog CRLR is 64.7%, and flounder CRLR is 61.2% and this was higher than to human calcitonin rec ...
... The receptors for calcitonin gene-related peptide (CGRP) and adrenomedullin (AM) are complexes of the calcitonin receptor-like receptor (CLR) and receptor activity-modifying proteins (RAMP). The CGRP receptor is a CLR/RAMP1 pairing whereas CLR/RAMP2 and CLR/RAMP3 constitute two subtypes of AM receptor: AM₁ and AM₂, respectively. Previous studies identified Glu74 in RAMP3 to be important for AM bin ...
... Investigations on "nonclassic" regulators of angiogenesis could open new perspectives in understanding angiogenesis under physiological and pathological conditions. A pro-angiogenic effect has been demonstrated for adrenomedullin (AM), it´s co-factor activity-modifying protein 2 (RAMP-2) and the calcitonin receptor-like receptor (CALCLR). This signalling pathway is besides associated with lymphang ...
... Radioligand binding assays of membrane fraction of the shell gland endometrium of guineafowl revealed the presence of receptor for calcitonin. The equilibrium dissociation constant (Kd) obtained by Scatchard analyses was 0.50 to 1.25 nM in laying birds and 1.12 to 1.19 nM in nonlaying birds. The maximum binding capacity (Bmax) per milligram of protein was 33.1 to 107.5 femtomoles in laying birds a ...