Introduction of CALCR

The calcitonin is a polypeptide hormone that is able to decrease blood calcium levels by direct inhibition of mediated bone resorption and by enhancing calcium excretion by the kidney. The activities of calcitonin are mediated by high-affinity calcitonin receptors (CTRs or CALCRs). The CALCR is a class B G-protein coupled receptor. This family of receptors is characterized by seven transmembrane segments connected by three extracellular loops. The human CALCR gene is located on chromosome 7. This receptor is able to couple at least two signal transduction pathways: the cAMP signal transduction and the phospholipase C enzyme pathway.

Functions of CALCR Membrane Protein

The CALCR receptors are highly expressed on osteoclasts and have been exploited therapeutically for treatment of bone disorders, including Paget’s disease, hypercalcemia of malignancy and osteoporosis. The receptors are also expressed in numerous other cells and tissues including leucocytes and their precursors, the central nervous system, kidney, lung, gastrointestinal tract and reproductive tissues, thereby influencing pain perception, feeding and reproduction, and ion secretion. Moreover, the polymorphisms of CALCR gene were reported to be implicated in different diseases. For example, it is associated with bone mineral density at the lumbar spine and may be used as a genetic marker for predicting the risk of developing osteoporosis. Besides, the CALCR polymorphism may be associated with kidney stone disease.

Applications of CALCR Membrane Protein in Literature

1. Dal E M, et al. Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy. Biochemical Pharmacology. 2018, 150: 214-244. PMID: 29454620

In this study, the extracellular loops (ECLs) 2 and 3 of the human calcitonin receptor have been mutated to interrogate receptor expression, peptide affinity, and efficacy for cAMP and IP1 accumulation, as well as pERK in response to calcitonin and related family peptides.

2. Dal E M, et al. Characterization of signalling and regulation of common calcitonin receptor splice variants and polymorphisms. Biochemical Pharmacology. 2017, 148: 111-129. PMID: 29277692

This study reported a robust, direct comparison of these human-specific splicing and polymorphic variants of calcitonin receptor, for their ability to activate distinct signaling pathways in response to different CTR ligands.

3. Andreassen K V, et al. A novel oral dual amylin and calcitonin receptor agonist (KBP-042) exerts antiobesity and antidiabetic effects in rats. American Journal of Physiology-Endocrinology and Metabolism. 2014, 307(1): E24-E33. PMID: 24801386

This study investigated a novel oral dual amylin and calcitonin receptor agonist, KBP-042, in comparison with salmon calcitonin with regard to in vitro receptor pharmacology, ex vivo pancreatic islet studies, and in vivo proof-of-concept studies in diet-induced obese and Zucker diabetic fatty rats. The results suggested KBP-042 as a novel therapeutic agent in type 2 diabetes.

4. Takano S, et al. Synovial macrophage-derived IL-1β regulates the calcitonin receptor in osteoarthritic mice. Clinical & Experimental Immunology. 2016, 183(1): 143-149. PMID: 26400621

To investigate the regulation of calcitonin gene-related peptide receptor signaling by macrophages in the synovial tissue (ST) of osteoarthritis (OA) joints, this study characterized the gene expression profiles of these receptors in the ST of OA mice. The study results suggested that synovial macrophages were the major producers of IL-1β and regulators of CLR in OA mice and that macrophages and IL-1β might be suitable therapeutic targets for treating OA pain.

5. Neuerburg C, et al. The role of calcitonin receptor signalling in polyethylene particle-induced osteolysis. Acta biomaterialia. 2015, 14: 125-132. PMID: 25486133

To uncover the role of direct calcitonin receptor-mediated signaling, this study investigated particle-induced osteolysis in a murine calvaria model with a global deletion of the calcitonin receptor.

CALCR Preparation Options

Creative Biolabs offers a wide range of membrane protein services for a great variety of applications and research areas. A variety of strategies and methods have been developed to solubilize membrane proteins for biophysical and biochemical analyses, namely detergents, nanodiscs, bicelles, liposomes, and amphipols. Each of these methods has advantages and disadvantages, and the selection of a “right” one should be on a sample-by-sample basis. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-CALCR antibody development services.

• Magic™ Membrane Protein Production Platform
• Magic™ Anti-Membrane Protein Antibody Discovery Platform

Our goal is to provide our customers with the best quality membrane targets, overcoming many difficulties in their structural and functional studies and further applications. We customize the service according to the specific requirements from the customers. Please do not hesitate to contact us for more details about our membrane protein preparation services.

All listed services and products are For Research Use Only. Do Not use in any diagnostic or therapeutic applications.