Page last updated: 2024-08-07 17:10:30

Calcitonin gene-related peptide type 1 receptor

A calcitonin gene-related peptide type 1 receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16602]

Synonyms

CGRP type 1 receptor;
Calcitonin receptor-like receptor

Research

Bioassay Publications (15)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (6.67)18.2507
2000's4 (26.67)29.6817
2010's9 (60.00)24.3611
2020's1 (6.67)2.80

Compounds (8)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
haloperidolHomo sapiens (human)Ki0.000411
azaperoneHomo sapiens (human)Ki0.052011
telcagepantHomo sapiens (human)IC500.00661010
telcagepantHomo sapiens (human)Ki0.000888
mk 3207Homo sapiens (human)Ki0.000033
bms 694153Homo sapiens (human)IC500.000011
bms 694153Homo sapiens (human)Ki0.000045
(5s,6s,9r)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5h-cyclohepta(b)pyridin-9-yl 4-(2-oxo-2,3-dihydro-1h-imidazo(4,5-b)pyridin-1-yl)piperidine-1-carboxylateHomo sapiens (human)Ki0.000011
mk-8825Homo sapiens (human)IC500.000322
mk-8825Homo sapiens (human)Ki5.147544
atogepantHomo sapiens (human)Ki0.000011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
telcagepantHomo sapiens (human)Kd0.002822
bms 694153Homo sapiens (human)EC500.000011
(5s,6s,9r)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5h-cyclohepta(b)pyridin-9-yl 4-(2-oxo-2,3-dihydro-1h-imidazo(4,5-b)pyridin-1-yl)piperidine-1-carboxylateHomo sapiens (human)EC500.000111
mk-8825Homo sapiens (human)Kd0.000111

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
bms 694153Homo sapiens (human)Kb0.000011
mk-8825Homo sapiens (human)Kb0.000111

Enables

This protein enables 6 target(s):

TargetCategoryDefinition
adrenomedullin receptor activitymolecular functionCombining with adrenomedullin to initiate a change in cell activity. [GOC:ai]
calcitonin gene-related peptide receptor activitymolecular functionCombining with a calcitonin gene-related polypeptide (CGRP) to initiate a change in cell activity. [GOC:mah, PMID:12037140]
G protein-coupled receptor activitymolecular functionCombining 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]
calcitonin receptor activitymolecular functionCombining with calcitonin 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:mah, GOC:signaling, PMID:21649645]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
adrenomedullin bindingmolecular functionBinding to adrenomedullin (AM). [GOC:bhm, PMID:10882736]

Located In

This protein is located in 5 target(s):

TargetCategoryDefinition
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
lysosomecellular componentA small lytic vacuole that has cell cycle-independent morphology found in most animal cells and that contains a variety of hydrolases, most of which have their maximal activities in the pH range 5-6. The contained enzymes display latency if properly isolated. About 40 different lysosomal hydrolases are known and lysosomes have a great variety of morphologies and functions. [GOC:mah, ISBN:0198506732]
endosomecellular componentA vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797]
endoplasmic reticulumcellular componentThe irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Part Of

This protein is part of 2 target(s):

TargetCategoryDefinition
adrenomedullin receptor complexcellular componentA transmembrane, G protein-coupled signaling receptor complex which is capable of adrenomedullin receptor activity. [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:22102369]
CGRP receptor complexcellular componentA transmembrane, G protein-coupled signaling receptor complex recognized by calcitonin gene-related peptides (CGRP). [GOC:bhm, PMID:20826335]

Involved In

This protein is involved in 13 target(s):

TargetCategoryDefinition
angiogenesisbiological processBlood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453]
calcium ion transportbiological processThe directed movement of calcium (Ca) ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai]
cell surface receptor signaling pathwaybiological processThe series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling]
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerbiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194]
adenylate cyclase-activating G protein-coupled receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194]
heart developmentbiological processThe process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948]
protein transportbiological processThe directed movement of proteins into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai]
receptor internalizationbiological processA receptor-mediated endocytosis process that results in the movement of receptors from the plasma membrane to the inside of the cell. The process begins when cell surface receptors are monoubiquitinated following ligand-induced activation. Receptors are subsequently taken up into endocytic vesicles from where they are either targeted to the lysosome or vacuole for degradation or recycled back to the plasma membrane. [GOC:bf, GOC:mah, GOC:signaling, PMID:15006537, PMID:19643732]
cellular response to sucrose stimulusbiological processAny 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 sucrose stimulus. [GOC:mah]
positive regulation of vascular associated smooth muscle cell proliferationbiological processAny process that activates or increases the frequency, rate or extent of vascular smooth muscle cell proliferation. [GO_REF:0000058, GOC:TermGenie, PMID:23246467]
calcitonin gene-related peptide receptor signaling pathwaybiological processThe series of molecular signals initiated by an extracellular calcitonin gene-related peptide (CGRP) combining with a calcitonin gene-related peptide receptor on the surface of the target cell. Calcitonin gene-related peptide receptors may form dimers, trimers or tetramers. [GOC:bhm, PMID:10882736]
adrenomedullin receptor signaling pathwaybiological processThe series of molecular signals initiated by an extracellular adrenomedullin combining with a dimeric adrenomedullin receptor on the surface of the target cell. [GOC:bhm, PMID:10882736]
vascular associated smooth muscle cell proliferationbiological processThe multiplication or reproduction of vascular smooth muscle cells, resulting in the expansion of a cell population. A vascular smooth muscle cell is a non-striated, elongated, spindle-shaped cell found lining the blood vessels. [PMID:23246467]