Property Summary

NCBI Gene PubMed Count 154
Grant Count 855
R01 Count 452
Funding $113,089,954.56
PubMed Score 684.60
PubTator Score 848.84

Knowledge Summary

Patent (21,409)

Expression

  Differential Expression (2)

Disease log2 FC p
psoriasis 1.300 0.001
osteosarcoma 1.578 0.000

Synonym

Accession P43220 Q2M229 Q99669 GLP-1 receptor
Symbols GLP-1
GLP-1R
GLP-1-R

Gene

PDB

3IOL   4ZGM   3C59   3C5T   5E94  

  TechDev Info (1)

MLP Assay (6)

AID Type Active / Inconclusive / Inactive Description
624148 confirmatory 2 / 47 / 1231 qHTS of GLP-1 Receptor Agonists: LOPAC Validation
624152 summary 0 / 0 / 0 qHTS of GLP-1 Receptor Agonists: Summary
624172 confirmatory 23 / 2833 / 372412 qHTS of GLP-1 Receptor Agonists
624417 confirmatory 6432 / 80185 / 321735 qHTS of GLP-1 Receptor Inverse Agonists (Inhibition Mode)
624421 summary 0 / 0 / 0 qHTS of GLP-1 Receptor Inverse Agonists: Summary
743262 confirmatory 23 / 112 / 1176 qHTS of GLP-1 Receptor Agonists: Hit Validation

Gene RIF (100)

PMID Text
27059958 The molecular dynamics simulations of wild-type and mutant GLP-1R.ligand complexes provided molecular insights into GLP-1R-specific recognition mechanisms for the N terminus of GLP-1 by residues in the 7TM pocket and explained how glucagon-mimicking GLP-1 mutants restored binding affinity for (glucagon receptor -mimicking) GLP-1R mutants.
26598711 NMR-determined structure of a high-potency cyclic conformationally-constrained 11-residue analogue of GLP-1 was also docked into the receptor-binding site.
26384381 Retinal GLP1R expression was similar in patients with diabetes and healthy controls.
26272612 a novel GLP1R Interacting Protein ATP6ap2
26238361 although GLP-1R is not an independent prognostic factor in PDAC patients, it appears to have some implications for pancreatic ductal adenocarcinoma metastatic ability
26198634 This study reveals the glucagon receptor as a previously unidentified target for GLP-1 receptor agonists and highlights a role for RAMP2 in regulating its pharmacology.
26116235 these findings demonstrate the hGLP-1R has distinct regions within the C-terminal domain required for its cell surface expression, activity and agonist-induced internalisation.
26080318 168Ser (rs6923761) was nominally associated with alcohol use disorder. The 168 Ser/Ser genotype was associated with increased alcohol administration, and with higher BOLD response in the right globus pallidus.
26015316 Lack of association of rs6923761 GLP-1 R polymorphism with weight loss.
25991051 GLP-1R rs10305420 polymorphism explained some of the inter-individual differences in response to liraglutide regarding weight loss in obese PCOS women.
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AA Sequence

MAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDLFCNRTFDEYA      1 - 70
CWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPWRDLSECEESKRGERSSPEEQ     71 - 140
LLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIHLNLFASFILRALSVFIKDAALKWMYSTAAQ    141 - 210
QHQWDGLLSYQDSLSCRLVFLLMQYCVAANYYWLLVEGVYLYTLLAFSVLSEQWIFRLYVSIGWGVPLLF    211 - 280
VVPWGIVKYLYEDEGCWTRNSNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLA    281 - 350
KSTLTLIPLLGTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERW    351 - 420
RLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS                               421 - 463
//

Text Mined References (156)

PMID Year Title
27068973 2016 The complexity of signalling mediated by the glucagon-like peptide-1 receptor.
27059958 2016 Structural Determinants of Binding the Seven-transmembrane Domain of the Glucagon-like Peptide-1 Receptor (GLP-1R).
27059816 2016 Differential effects of once-weekly glucagon-like peptide-1 receptor agonist dulaglutide and metformin on pancreatic ?-cell and insulin sensitivity during a standardized test meal in patients with type 2 diabetes.
27059784 2016 Allosteric Optical Control of a Class B G-Protein-Coupled Receptor.
27043162 2016 Postprandial plasma glucose effects of once-weekly albiglutide for the treatment of type 2 diabetes.
27042424 Glucagon-like peptide-1 receptor agonists in the treatment of type 2 diabetes: Past, present, and future.
27038451 2016 Acute renal effects of the GLP-1 receptor agonist exenatide in overweight type 2 diabetes patients: a randomised, double-blind, placebo-controlled trial.
27037787 2016 Adverse effects of incretin-based therapies on major cardiovascular and arrhythmia events: meta-analysis of randomized trials.
27037706 2016 Safety and Tolerability of Glucagon-Like Peptide-1 Receptor Agonists Utilizing Data from the Exenatide Clinical Trial Development Program.
27013681 2016 Astrocytes Regulate GLP-1 Receptor-Mediated Effects on Energy Balance.
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