Proteins > Glucagon-like peptide 1 receptor
Page last updated: 2024-08-07 13:17:39
Glucagon-like peptide 1 receptor
A glucagon-like peptide 1 receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:P43220]
Synonyms
GLP-1 receptor;
GLP-1-R;
GLP-1R
Research
Bioassay Publications (23)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 5 (21.74) | 29.6817 |
| 2010's | 12 (52.17) | 24.3611 |
| 2020's | 6 (26.09) | 2.80 |
Compounds (5)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Synthesis and biological evaluation of glucagon-like peptide-1 analogs with the C-terminal helix 3 of albumin-binding domain 3.Bioorganic & medicinal chemistry, , 05-15, Volume: 62, 2022
A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Novel lipid side chain modified exenatide analogs emerged prolonged glucoregulatory activity and potential body weight management properties.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Design, synthesis, and biological activity of novel dicoumarol glucagon-like peptide 1 conjugates.Journal of medicinal chemistry, , Dec-27, Volume: 56, Issue:24, 2013
Peptide-based long-acting co-agonists of GLP-1 and cholecystokinin 1 receptors as novel anti-diabesity agents.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Modifying a Hydroxyl Patch in Glucagon-like Peptide 1 Produces Biased Agonists with Unique Signaling Profiles.Journal of medicinal chemistry, , 09-08, Volume: 65, Issue:17, 2022
Discovery of MK-1462: GLP-1 and Glucagon Receptor Dual Agonist for the Treatment of Obesity and Diabetes.ACS medicinal chemistry letters, , Aug-11, Volume: 13, Issue:8, 2022
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Peptide Half-Life Extension: Divalent, Small-Molecule Albumin Interactions Direct the Systemic Properties of Glucagon-Like Peptide 1 (GLP-1) Analogues.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Design of Novel Exendin-Based Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists.Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Design, synthesis, and biological activity of novel dicoumarol glucagon-like peptide 1 conjugates.Journal of medicinal chemistry, , Dec-27, Volume: 56, Issue:24, 2013
A general method for making peptide therapeutics resistant to serine protease degradation: application to dipeptidyl peptidase IV substrates.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7-36) analog.Bioorganic & medicinal chemistry letters, , Sep-06, Volume: 14, Issue:17, 2004
Modifying a Hydroxyl Patch in Glucagon-like Peptide 1 Produces Biased Agonists with Unique Signaling Profiles.Journal of medicinal chemistry, , 09-08, Volume: 65, Issue:17, 2022
A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Design and Evaluation of Peptide Dual-Agonists of GLP-1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis.Journal of medicinal chemistry, , 01-28, Volume: 64, Issue:2, 2021
Novel lipid side chain modified exenatide analogs emerged prolonged glucoregulatory activity and potential body weight management properties.Bioorganic & medicinal chemistry, , 10-15, Volume: 27, Issue:20, 2019
Novel fatty acid chain modified GLP-1 derivatives with prolonged in vivo glucose-lowering ability and balanced glucoregulatory activity.Bioorganic & medicinal chemistry, , 05-15, Volume: 26, Issue:9, 2018
Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multidose Formulations.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
Design of Novel Exendin-Based Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists.Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Design, synthesis, and biological activity of novel dicoumarol glucagon-like peptide 1 conjugates.Journal of medicinal chemistry, , Dec-27, Volume: 56, Issue:24, 2013
Identification of glycosylated exendin-4 analogue with prolonged blood glucose-lowering activity through glycosylation scanning substitution.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity.Journal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
A novel glucagon-like peptide-1/glucagon receptor dual agonist exhibits weight-lowering and diabetes-protective effects.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide.Journal of medicinal chemistry, , Sep-24, Volume: 58, Issue:18, 2015
Small-molecule agonists for the glucagon-like peptide 1 receptor.Proceedings of the National Academy of Sciences of the United States of America, , Jan-16, Volume: 104, Issue:3, 2007
Potent derivatives of glucagon-like peptide-1 with pharmacokinetic properties suitable for once daily administration.Journal of medicinal chemistry, , May-04, Volume: 43, Issue:9, 2000
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| transmembrane signaling receptor activity | molecular function | Combining with an extracellular or intracellular signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity or state as part of signal transduction. [GOC:go_curators, Wikipedia:Transmembrane_receptor] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| glucagon-like peptide 1 receptor activity | molecular function | Combining with glucagon-like peptide 1 and transmitting the signal across the membrane by activating an associated G-protein. [GOC:jl, PMID:12529935] |
| peptide hormone binding | molecular function | Binding to a peptide with hormonal activity in animals. [GOC:jl, ISBN:0198506732] |
| glucagon receptor activity | molecular function | Combining with glucagon 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:22438981] |
Located In
This protein is located in 2 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] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
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 13 target(s):
| Target | Category | Definition |
|---|
| 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] |
| 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] |
| activation of adenylate cyclase activity | biological process | Any process that initiates the activity of the inactive enzyme adenylate cyclase. [GOC:ai] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| learning or memory | biological process | The acquisition and processing of information and/or the storage and retrieval of this information over time. [GOC:jid, PMID:8938125] |
| regulation of heart contraction | biological process | Any process that modulates the frequency, rate or extent of heart contraction. Heart contraction is the process in which the heart decreases in volume in a characteristic way to propel blood through the body. [GOC:dph, GOC:go_curators, GOC:tb] |
| cAMP-mediated signaling | biological process | An intracellular signaling cassette that starts with production of cyclic AMP (cAMP), and ends with activation of downstream effectors that further transmit the signal within the cell. [GOC:signaling] |
| post-translational protein targeting to membrane, translocation | biological process | The process in which a protein translocates through the ER membrane posttranslationally. [PMID:12518317, PMID:8707814] |
| negative regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is decreased. [GOC:go_curators, GOC:mtg_cardio] |
| hormone secretion | biological process | The regulated release of hormones, substances with a specific regulatory effect on a particular organ or group of cells. [ISBN:0198506732] |
| cellular response to glucagon 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 glucagon stimulus. [GOC:mah] |
| response to psychosocial stress | 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 exposure to aversive or demanding psychological and social conditions that tax or exceed the behavioral resources of the organism. [PMID:22922217, PMID:26458179] |
| positive regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is increased. [GOC:go_curators, GOC:mtg_cardio] |