Property Summary

NCBI Gene PubMed Count 40
Grant Count 111
R01 Count 81
Funding $10,667,913.2
PubMed Score 149.48
PubTator Score 236.28

Knowledge Summary

Patent (64,408)

Expression

Synonym

Accession P47871 Q2M3M5 GL-R
Symbols GGR
GL-R

Gene

PDB

2A83   3CZF   4ERS   4L6R   4LF3   5EE7  

  TechDev Info (1)

Gene RIF (22)

PMID Text
27111510 2.5 A crystal structure of human GCGR in complex with the antagonist MK-0893, which is found to bind to an allosteric site outside the seven transmembrane helical bundle in a position between TM6 and TM7 extending into the lipid bilayer
26227798 Molecular dynamics and disulfide crosslinking studies suggest that apo-GCGR can adopt both an open and closed conformation associated with extensive contacts between the ECD and 7TM domain. Glucagon binds to GCGR by a conformational selection mechanism.
25695890 glucagon cell adenomatosis with GCGR germline mutations seems to follow an autosomal-recessive trait.
25451942 Using a real-time time-resolved FRET-based internalization assay, we show that GLP-1R, GIPR, and GCGR internalize with differential properties
23863937 crystal structure of the seven transmembrane helical domain of human GCGR at 3.4 A resolution, and a hybrid model of glucagon bound to GCGR to understand the molecular recognition of the receptor for its native ligand
23407487 Letter/Case Report: nonfunctional glucagon cell adenomatosis with no detectable glucagon receptor mutations.
23185367 GRA1 is a potent glucagon receptor antagonist with strong antihyperglycemic efficacy in preclinical models and prominent effects on hepatic gene-expression related to amino acid metabolism
22893257 F22, V23, M27, and D15 of GCGR are the most important residues for glucagon binding.
22438981 in addition to activation of the classic cAMP/protein kinase A (PKA) pathway, activation of GCGR also induced beta-catenin stabilization and activated beta-catenin-mediated transcription
22119466 analysis of glucagon receptor antagonists with reduced molecular weight and lipophilicity
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AA Sequence

MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPD      1 - 70
TPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSS     71 - 140
FQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDL    141 - 210
SVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVV    211 - 280
PWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKS    281 - 350
TLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL    351 - 420
GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF                 421 - 477
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Text Mined References (44)

PMID Year Title
27111510 2016 Extra-helical binding site of a glucagon receptor antagonist.
26227798 2015 Conformational states of the full-length glucagon receptor.
25695890 2015 Glucagon cell hyperplasia and neoplasia with and without glucagon receptor mutations.
25451942 2015 Functional consequences of glucagon-like peptide-1 receptor cross-talk and trafficking.
24749050 2014 Action and therapeutic potential of oxyntomodulin.
24527772 2014 The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
24359917 2014 Insights into the structure of class B GPCRs.
24275569 2014 An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome.
23863937 2013 Structure of the human glucagon class B G-protein-coupled receptor.
23407487 2013 Glucagon cell adenomatosis without glucagon receptor mutation.
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