Proteins > Calcitonin gene-related peptide type 1 receptor
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)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (6.67) | 18.2507 |
| 2000's | 4 (26.67) | 29.6817 |
| 2010's | 9 (60.00) | 24.3611 |
| 2020's | 1 (6.67) | 2.80 |
Compounds (8)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bms 694153 | Homo sapiens (human) | Kb | 0.0000 | 1 | 1 |
| mk-8825 | Homo sapiens (human) | Kb | 0.0001 | 1 | 1 |
Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migrBioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 19, Issue:22, 2009
Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-ylJournal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.ACS medicinal chemistry letters, , Sep-12, Volume: 4, Issue:9, 2013
Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migrBioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migrBioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 23, Issue:20, 2013
Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptidJournal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Discovery of (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-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in cJournal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| adrenomedullin receptor activity | molecular function | Combining with adrenomedullin to initiate a change in cell activity. [GOC:ai] |
| calcitonin gene-related peptide receptor activity | molecular function | Combining with a calcitonin gene-related polypeptide (CGRP) to initiate a change in cell activity. [GOC:mah, PMID:12037140] |
| 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] |
| calcitonin receptor activity | molecular function | Combining 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 binding | molecular function | Binding to a protein. [GOC:go_curators] |
| adrenomedullin binding | molecular function | Binding to adrenomedullin (AM). [GOC:bhm, PMID:10882736] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| lysosome | cellular component | A 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] |
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| endoplasmic reticulum | cellular component | The 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 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] |
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] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| adrenomedullin receptor complex | cellular component | A 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 complex | cellular component | A 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):
| Target | Category | Definition |
|---|
| angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
| calcium ion transport | biological process | The 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 pathway | biological process | The 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 messenger | biological process | A 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 pathway | biological process | A 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 development | biological process | The 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 transport | biological process | The 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 internalization | biological process | A 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 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 sucrose stimulus. [GOC:mah] |
| positive regulation of vascular associated smooth muscle cell proliferation | biological process | Any 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 pathway | biological process | The 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 pathway | biological process | The 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 proliferation | biological process | The 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] |