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Calcitonin GPCR Family Subtypes and Products

What Are Calcitonin Receptors?

Calcitonin receptors are a family of G protein-coupled receptors (GPCRs) generated by the CALCRL and CALCR genes, and contains four subtypes of receptors: calcitonin (CT), calcitonin gene-related peptide (CGRP), adrenomedullin (AM), and amylin (AMY) receptors. In conjunction with receptor activity-modifying proteins (RAMPs), the receptor’s function is changed. The RAMP family is comprised of three members: RAMP1, RAMP2, and RAMP3. Known agonists include ɑ-CGRP, β-CGRP, amylin, adrenemedullin, adrenomedullin 2/intermedin, and calcitonin. Known antagonists include olcegepant and telcagepant.

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Calcitonin Receptor Information

Clickable Text Interaction

CALCRL

CGRP/AM1/AM2

CT

AMY1/AMY2/AMY3

CALCRL (Calcitonin gene-related peptide type 1 receptor) is a receptor for calcitonin-gene-related peptide (CGRP) in the presence of the receptor activity modifying protein 1 (RAMP1) and receptor for adrenomedullin in the presence of RAMP2 or RAMP3. CALCRL is predominantly expressed in the lung and heart. The receptor is considered as a potential target for anti-migraine drugs.

The function and pharmacology of CALCRL receptor is modified in the presence of receptor activity-modifying proteins (RAMPs), which are single Transmembrane domain proteins of about 160 amino acids, having three isoforms: RAMP1, RAMP2 and RAMP3. CALCR can function either as a calcitonin gene-related peptide (CGRP) receptor or an adrenomedullin (AM) receptor, depending on which members of RAMPs, are co-expressed. The CALCRL/RAMP1 complex has been known as the CGRP receptor and has a very high affinity for CGRP. The CALCRL/RAMP2 complex has been known as the adrenomedullin (AM1) receptor. The CALCRL/RAMP3 complex has been known as the adrenomedullin (AM2) receptor.

CT is expressed in brain, bone, stomach, intestine, kidney and testes. Data from transgenic mice support a major role for calcitonin and its receptor in the formation and resorption aspects of bone metabolism under physiological conditions.

Amylin receptors are multimeric complexes and have been closely associated with Calcitonin receptor (CT). CT, in the presence of the receptor activity modifying proteins (RAMP1, RAMP2 and RAMP3), forms pharmacologically distinct Amylin subtypes (AMY1, AMY2 and AMY3) which acts as a high affinity receptor for amylin, a hormone secrete by B cell of pancreas that has a major role in glucose regulation.

Calcitonin Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
CalcitoninCALCRLhumanHEK293TC1232DC1232MC1232
CALCRLhumanCHO-K1C1232-1DC1232-1MC1232-1
CGRPhumanCHO-K1C1515-1DC1515-1MC1515-1
AM1humanCHO-K1C1516-1DC1516-1MC1516-1
AM2humanCHO-K1C1517-1DC1517-1MC1517-1
CThumanHEK293TH1231DH1231MH1231
CThumanCHO-K1C1231-1ADC1231-1AMC1231-1A
CThumanCHO-K1C1231-1BDC1231-1BMC1231-1B
AMY1humanCHO-K1C1509-1DC1509-1MC1509-1
AMY1humanCHO-K1C1509-1aDC1509-1aMC1509-1a
AMY2humanCHO-K1C1510-1aDC1510-1aMC1510-1a
AMY2humanCHO-K1C1510-1bDC1510-1bMC1510-1b
AMY3humanCHO-K1C1511-1aDC1511-1aMC1511-1a

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