Extracellular calcium-sensing receptor

An extracellular calcium-sensing receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P41180]

Synonyms

CaR;
CaSR;
hCasR;
Parathyroid cell calcium-sensing receptor 1;
PCaR1

Research

Bioassay Publications (12)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	6 (50.00)	29.6817
2010's	6 (50.00)	24.3611
2020's	0 (0.00)	2.80

Compounds (7)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
nps2143	Homo sapiens (human)	IC50	0.0285	8	8
ronacaleret	Homo sapiens (human)	IC50	0.1460	1	1

Drugs with Activation Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
fendiline	Homo sapiens (human)	EC50	1.0000	1	1
cinacalcet hydrochloride	Homo sapiens (human)	EC50	0.1000	2	2
cinacalcet	Homo sapiens (human)	EC50	0.0800	1	1
nps-568	Homo sapiens (human)	EC50	0.0800	1	1
nps-568	Homo sapiens (human)	EC50	0.1370	2	2

Enables

This protein enables 9 target(s):

Target	Category	Definition
phosphatidylinositol phospholipase C activity	molecular function	Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate + H2O = 1,2-diacylglycerol + 1D-myo-inositol 1,4,5-trisphosphate + H+. [EC:3.1.4.11, RHEA:33179]
G protein-coupled receptor activity	molecular function	Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR]
integrin binding	molecular function	Binding to an integrin. [GOC:ceb]
calcium ion binding	molecular function	Binding to a calcium ion (Ca2+). [GOC:ai]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
amino acid binding	molecular function	Binding to an amino acid, organic acids containing one or more amino substituents. [GOC:ai]
protein kinase binding	molecular function	Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl]
protein homodimerization activity	molecular function	Binding to an identical protein to form a homodimer. [GOC:jl]
transmembrane transporter binding	molecular function	Binding to a transmembrane transporter, a protein or protein complex that enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:BHF, GOC:jl, PMID:33199372]

Located In

This protein is located in 6 target(s):

Target	Category	Definition
plasma membrane	cellular component	The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
cell surface	cellular component	The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm]
basolateral plasma membrane	cellular component	The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators]
apical plasma membrane	cellular component	The region of the plasma membrane located at the apical end of the cell. [GOC:curators]
neuronal cell body	cellular component	The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators]
axon terminus	cellular component	Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal button is a specialized region of it. [GOC:dph, GOC:jl]

Active In

This protein is active in 1 target(s):

Target	Category	Definition
plasma membrane	cellular component	The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Involved In

This protein is involved in 31 target(s):

Target	Category	Definition
ossification	biological process	The formation of bone or of a bony substance, or the conversion of fibrous tissue or of cartilage into bone or a bony substance. [GOC:mtg_mpo, PMID:17572649]
response to ischemia	biological process	Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a inadequate blood supply. [GOC:hjd]
detection of calcium ion	biological process	The series of events in which a calcium ion stimulus is received by a cell and converted into a molecular signal. [GOC:pg]
intracellular calcium ion homeostasis	biological process	A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah]
G protein-coupled receptor signaling pathway	biological process	The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor]
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	biological process	A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194]
phospholipase C-activating G protein-coupled receptor signaling pathway	biological process	A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194]
JNK cascade	biological process	A MAPK cascade containing at least the JNK (MAPK8) MAP kinase. It starts with the activation of JUN3K (a MAPK3K), which activates JNKK a MAP2K), which in turn activates JNK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinases in the downstream tier. The JNK cascade is activated by stress signals, as well as by G protein-coupled receptors, growth factors, and cytokines, and results in cellular responses such as cell proliferation, cell differentiation, apoptosis and inflammation. [PMID:11790549, PMID:20811974, PMID:23125017]
chemosensory behavior	biological process	Behavior that is dependent upon the sensation of chemicals. [GOC:go_curators]
positive regulation of cell population proliferation	biological process	Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators]
anatomical structure morphogenesis	biological process	The process in which anatomical structures are generated and organized. Morphogenesis pertains to the creation of form. [GOC:go_curators, ISBN:0521436125]
positive regulation of gene expression	biological process	Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018]
positive regulation of insulin secretion	biological process	Any process that activates or increases the frequency, rate or extent of the regulated release of insulin. [GOC:mah]
bile acid secretion	biological process	The regulated release of bile acid, composed of any of a group of steroid carboxylic acids occurring in bile, by a cell or a tissue. [GOC:ecd]
cellular response to hepatocyte growth factor stimulus	biological process	Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hepatocyte growth factor stimulus. [GOC:bf]
vasodilation	biological process	An increase in the internal diameter of blood vessels, especially arterioles or capillaries, due to relaxation of smooth muscle cells that line the vessels, and usually resulting in a decrease in blood pressure. [GOC:pr, ISBN:0192800981]
positive regulation of vasoconstriction	biological process	Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators]
branching morphogenesis of an epithelial tube	biological process	The process in which the anatomical structures of branches in an epithelial tube are generated and organized. A tube is a long hollow cylinder. [GOC:dgh, GOC:dph, GOC:jid]
positive regulation of positive chemotaxis	biological process	Any process that activates or increases the frequency, rate or extent of the directed movement of a motile cell or organism towards a higher concentration in a concentration gradient of a specific chemical. [GOC:ai]
fat pad development	biological process	The progression of a fat pad from its initial formation to its mature structure. A fat pad is an accumulation of adipose tissue. [GOC:dph]
positive regulation of ERK1 and ERK2 cascade	biological process	Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah]
calcium ion import	biological process	The directed movement of calcium ions into a cell or organelle. [GOC:mah]
cellular response to vitamin D	biological process	Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a vitamin D stimulus. [GOC:mah]
cellular response to glucose stimulus	biological process	Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a glucose stimulus. [GOC:mah]
cellular response to low-density lipoprotein particle stimulus	biological process	Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a low-density lipoprotein particle stimulus. [GOC:mah]
cellular response to hypoxia	biological process	Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah]
response to fibroblast growth factor	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a fibroblast growth factor stimulus. [GOC:mah]
positive regulation of calcium ion import	biological process	Any process that increases the rate, frequency, or extent of the directed movement of calcium ions into a cell or organelle. [GOC:BHF]
cellular response to peptide	biological process	Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a peptide stimulus. [GOC:pr, GOC:TermGenie]
chloride transmembrane transport	biological process	The process in which chloride is transported across a membrane. [GOC:TermGenie, GOC:vw]
regulation of calcium ion transport	biological process	Any process that modulates the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai]

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