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6XOX

cryo-EM of human GLP-1R bound to non-peptide agonist LY3502970

Functional Information from GO Data
ChainGOidnamespacecontents
A0002862biological_processnegative regulation of inflammatory response to antigenic stimulus
A0003091biological_processrenal water homeostasis
A0003924molecular_functionGTPase activity
A0003925molecular_functionG protein activity
A0005515molecular_functionprotein binding
A0005525molecular_functionGTP binding
A0005737cellular_componentcytoplasm
A0005829cellular_componentcytosol
A0005834cellular_componentheterotrimeric G-protein complex
A0005886cellular_componentplasma membrane
A0007165biological_processsignal transduction
A0007186biological_processG protein-coupled receptor signaling pathway
A0007189biological_processadenylate cyclase-activating G protein-coupled receptor signaling pathway
A0007190biological_processactivation of adenylate cyclase activity
A0007191biological_processadenylate cyclase-activating dopamine receptor signaling pathway
A0007608biological_processsensory perception of smell
A0010856molecular_functionadenylate cyclase activator activity
A0016020cellular_componentmembrane
A0019001molecular_functionguanyl nucleotide binding
A0031683molecular_functionG-protein beta/gamma-subunit complex binding
A0031748molecular_functionD1 dopamine receptor binding
A0032588cellular_componenttrans-Golgi network membrane
A0046872molecular_functionmetal ion binding
A0046907biological_processintracellular transport
A0048589biological_processdevelopmental growth
A0050796biological_processregulation of insulin secretion
A0050890biological_processcognition
A0060348biological_processbone development
A0060789biological_processhair follicle placode formation
A0070062cellular_componentextracellular exosome
A0070527biological_processplatelet aggregation
A0071377biological_processcellular response to glucagon stimulus
A0071380biological_processcellular response to prostaglandin E stimulus
A0071870biological_processcellular response to catecholamine stimulus
A0071880biological_processadenylate cyclase-activating adrenergic receptor signaling pathway
A0120162biological_processpositive regulation of cold-induced thermogenesis
B0001750cellular_componentphotoreceptor outer segment
B0003924molecular_functionGTPase activity
B0005515molecular_functionprotein binding
B0005737cellular_componentcytoplasm
B0005765cellular_componentlysosomal membrane
B0005829cellular_componentcytosol
B0005834cellular_componentheterotrimeric G-protein complex
B0005886cellular_componentplasma membrane
B0007165biological_processsignal transduction
B0007186biological_processG protein-coupled receptor signaling pathway
B0007191biological_processadenylate cyclase-activating dopamine receptor signaling pathway
B0007200biological_processphospholipase C-activating G protein-coupled receptor signaling pathway
B0007213biological_processG protein-coupled acetylcholine receptor signaling pathway
B0007265biological_processRas protein signal transduction
B0008283biological_processcell population proliferation
B0016020cellular_componentmembrane
B0030159molecular_functionsignaling receptor complex adaptor activity
B0044877molecular_functionprotein-containing complex binding
B0045202cellular_componentsynapse
B0050909biological_processsensory perception of taste
B0051020molecular_functionGTPase binding
B0060041biological_processretina development in camera-type eye
B0070062cellular_componentextracellular exosome
B0071380biological_processcellular response to prostaglandin E stimulus
B0071870biological_processcellular response to catecholamine stimulus
B0097381cellular_componentphotoreceptor disc membrane
B1903561cellular_componentextracellular vesicle
G0005515molecular_functionprotein binding
G0005834cellular_componentheterotrimeric G-protein complex
G0005886cellular_componentplasma membrane
G0007165biological_processsignal transduction
G0007186biological_processG protein-coupled receptor signaling pathway
G0007191biological_processadenylate cyclase-activating dopamine receptor signaling pathway
G0016020cellular_componentmembrane
G0031681molecular_functionG-protein beta-subunit binding
G0048144biological_processfibroblast proliferation
G0070062cellular_componentextracellular exosome
G0071380biological_processcellular response to prostaglandin E stimulus
G0071870biological_processcellular response to catecholamine stimulus
R0004888molecular_functiontransmembrane signaling receptor activity
R0004930molecular_functionG protein-coupled receptor activity
R0004967molecular_functionglucagon receptor activity
R0005515molecular_functionprotein binding
R0005886cellular_componentplasma membrane
R0007166biological_processcell surface receptor signaling pathway
R0007186biological_processG protein-coupled receptor signaling pathway
R0007189biological_processadenylate cyclase-activating G protein-coupled receptor signaling pathway
R0007190biological_processactivation of adenylate cyclase activity
R0007204biological_processpositive regulation of cytosolic calcium ion concentration
R0007611biological_processlearning or memory
R0008016biological_processregulation of heart contraction
R0008528molecular_functionG protein-coupled peptide receptor activity
R0016020cellular_componentmembrane
R0017046molecular_functionpeptide hormone binding
R0019933biological_processcAMP-mediated signaling
R0031204biological_processpost-translational protein targeting to membrane, translocation
R0038023molecular_functionsignaling receptor activity
R0044508molecular_functionglucagon-like peptide 1 receptor activity
R0045776biological_processnegative regulation of blood pressure
R0045777biological_processpositive regulation of blood pressure
R0046879biological_processhormone secretion
R0071377biological_processcellular response to glucagon stimulus
R1990911biological_processresponse to psychosocial stress
Functional Information from PDB Data
site_idAC1
Number of Residues12
Detailsbinding site for residue V6G R 501
ChainResidue
RSER31
RCYS226
RPHE230
RLEU388
RTRP33
RLEU141
RLEU144
RTYR145
RLYS197
RLEU201
RTYR205
RTYR220

Functional Information from PROSITE/UniProt
site_idPS00649
Number of Residues25
DetailsG_PROTEIN_RECEP_F2_1 G-protein coupled receptors family 2 signature 1. CnrtFDeya.CWpdGepgsfvnvsCP
ChainResidueDetails
RCYS62-PRO86

site_idPS00650
Number of Residues16
DetailsG_PROTEIN_RECEP_F2_2 G-protein coupled receptors family 2 signature 2. QGLMVaILYCFvNneV
ChainResidueDetails
RGLN394-VAL409

site_idPS00678
Number of Residues15
DetailsWD_REPEATS_1 Trp-Asp (WD) repeats signature. LVSAsqDgKLIIWDS
ChainResidueDetails
BLEU70-SER84
BILE157-ILE171
BLEU285-ALA299

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues166
DetailsTOPO_DOM: Extracellular => ECO:0000269|PubMed:28514449
ChainResidueDetails
RARG24-GLU139
AARG380
RLYS202-ARG227
RTYR291-TYR305
RMET371-LYS383
ASER54
ALYS211
AASN218
ACYS237
ASER306

site_idSWS_FT_FI2
Number of Residues24
DetailsTRANSMEM: Helical; Name=1 => ECO:0000269|PubMed:28514449
ChainResidueDetails
RGLN140-ALA164
AASN292

site_idSWS_FT_FI3
Number of Residues42
DetailsTOPO_DOM: Cytoplasmic => ECO:0000269|PubMed:28514449
ChainResidueDetails
RILE165-THR175
RTYR252-ILE265
RCYS329-ARG348

site_idSWS_FT_FI4
Number of Residues25
DetailsTRANSMEM: Helical; Name=2 => ECO:0000269|PubMed:28514449
ChainResidueDetails
RARG176-LEU201
AALA366

site_idSWS_FT_FI5
Number of Residues23
DetailsTRANSMEM: Helical; Name=3 => ECO:0000269|PubMed:28514449
ChainResidueDetails
RLEU228-LEU251

site_idSWS_FT_FI6
Number of Residues24
DetailsTRANSMEM: Helical; Name=4 => ECO:0000269|PubMed:28514449
ChainResidueDetails
RPHE266-LEU290

site_idSWS_FT_FI7
Number of Residues22
DetailsTRANSMEM: Helical; Name=5 => ECO:0000269|PubMed:28514449
ChainResidueDetails
RTRP306-ILE328

site_idSWS_FT_FI8
Number of Residues21
DetailsTRANSMEM: Helical; Name=6 => ECO:0000269|PubMed:28514449
ChainResidueDetails
RLEU349-VAL370

site_idSWS_FT_FI9
Number of Residues20
DetailsTRANSMEM: Helical; Name=7 => ECO:0000269|PubMed:28514449
ChainResidueDetails
RLEU384-PHE404

site_idSWS_FT_FI10
Number of Residues2
DetailsSITE: Interaction with the endogenous ligand GLP-1 => ECO:0000269|PubMed:19861722
ChainResidueDetails
RARG121
RGLU128

site_idSWS_FT_FI11
Number of Residues1
DetailsMOD_RES: ADP-ribosylcysteine => ECO:0000269|PubMed:21901419
ChainResidueDetails
RCYS341

site_idSWS_FT_FI12
Number of Residues1
DetailsMOD_RES: ADP-ribosylarginine => ECO:0000269|PubMed:21901419
ChainResidueDetails
RARG348

site_idSWS_FT_FI13
Number of Residues3
DetailsCARBOHYD: N-linked (GlcNAc...) asparagine => ECO:0000269|PubMed:22412906
ChainResidueDetails
RASN63
RASN82
RASN115

219140

PDB entries from 2024-05-01

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