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Calcitonin GPCR Assays

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Introduction of Calcitonin Receptor (CTR)

The calcitonin (CT) peptide family is composed of diverse members whose receptors are biologically important for many diseases, including migraine, obesity, diabetes, osteoporosis, hypercalcemia, and cardiovascular-related diseases. Calcitonin receptor (CTR) and calcitonin receptor-like receptor (CLR) are two of the human class B1 group G protein-coupled receptors (GPCRs). CTRs and CLRs are of vital importance in biology because their pharmacology is closely linked to receptor activity modifying protein interactions.

Calcitonin gene-related peptide receptor.Fig.1. Calcitonin gene-related peptide receptor. (Camara, 2021)

Distribution and Function of CTRs

CTR is widely expressed in many tissues, including reproductive organs, gastrointestinal kidneys, lungs, and the brain. CTRs are closely related to the activation regulation of calcium homeostasis and bone turnover. Therefore, CTRs have emerged as attractive targets for the treatment of a variety of bone diseases caused by abnormal bone turnover and calcium regulation, including malignant osteoporosis, hypercalcemia, and Paget's disease.

Subtypes and Mechanisms of CTRs

CTRs play an important role in a variety of diseases. The main information about calcitonin and related receptors is summarized as follows:

Receptor Gene Mechanism Agonists Antagonists
Calcitonin receptor CALCR
  • CTR coupling to Gs proteins stimulates AC and increases cAMP in cells.
  • αCGRP
  • Adrenomedullin 2
  • Amylin
  • Calcitonin
  • SUN-B 8155
  • AC 187
  • BIBN 4096
  • CGRP 8-37
  • SB 268262
Calcitonin receptor-like receptor CALCRL
  • CLR participates in TxA-induced MAP kinase activation.
  • αCGRP
  • SUN-B 8155
  • SB 268262

Assay List of Calcitonin Receptors

Creative Biolabs can provide a range of assays of calcitonin receptors. You can choose the assay in the list or contact us for more information:

CALCR CALCRL
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX249 Magic™ Human CALCR (CTR/RAMP1) In Vitro cAMP Assay U2OS cAMP Assay
S01YF-1122-KX250 Magic™ Human CALCR (CTR/RAMP2) In Vitro cAMP Assay U2OS cAMP Assay
S01YF-1122-KX251 Magic™ Human CALCR (CTR/RAMP3) In Vitro cAMP Assay U2OS cAMP Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX246 Magic™ Human CALCRL (CLR/RAMP3) In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX252 Magic™ Human CALCRL (CRLR/RAMP1) In Vitro Calcium Flux Assay CHO-K1-Gqs Calcium Flux Assay
Radioligand Binding Assay
S01YF-1122-KX248 Magic™ Human CALCRL (CLR/RAMP3) In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX254 Magic™ Human CALCRL (CRLR/RAMP1) In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay

Published Data

Paper Title Calcitonin receptor signaling in the medial preoptic area enables risk-taking maternal care
Journal Cell Reports
Published 2021
Abstract In mammals, mothers typically exhibit more frequent offspring caregiving behavior, and the underlying mechanisms are currently unclear. The researchers found that CTR and its ligand amylin are expressed in distinct neuronal populations in the medial preoptic area (MPOA) and are upregulated in the mother. CTR+MPOA neurons are activated to somatomotor and monoaminergic brainstem nuclei by the parental care program. Retrograde monosynaptic tracing revealed marked changes in the afferents of CTR+neurons in the mother.
Result In this study, the researchers identified CTR as a molecular marker of activated cMPOA neurons through cultured behavior. Specific neuronal silencing experiments demonstrate that CTR+cMPOA neurons are closely linked to both maternal and allogeneic behavior. The findings suggest that the knockdown of CTR or amylin gene expression adversely affects risky maternal care, and specific silencing of CTR+MPOA neurons negatively affects parenting behavior. These data suggest that both maternal and allogeneic parenting behaviors are dependent on CTR+MPOA neurons, and that upregulation of amylin-CTR signaling in MPOA is at least in part associated with risky maternal care.

CTR ligand amylin is expressed in distinct MPOA neurons and upregulated during the lactation period.Fig.2. CTR ligand amylin is expressed in distinct MPOA neurons and upregulated during the lactation period. (Yoshihara, 2021)

References

  1. Camara, M. S.; et al. Epigenetic changes in headache. Neurología. 2021; 36(5): 369-376.
  2. Yoshihara, C.; et al. Epigenetic changes in headache. Cell Reports. 2021; 35(9): 109204.
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