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8POK

Cryo-EM structure of cell-free synthesized human histamine H2 receptor coupled to heterotrimeric Gs protein in lipid environment

Functional Information from GO Data
ChainGOidnamespacecontents
A0001696biological_processgastric acid secretion
A0004930molecular_functionG protein-coupled receptor activity
A0004969molecular_functionhistamine receptor activity
A0005886cellular_componentplasma membrane
A0006955biological_processimmune response
A0007186biological_processG protein-coupled receptor signaling pathway
A0007187biological_processG protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
A0007268biological_processchemical synaptic transmission
A0016020cellular_componentmembrane
A0030425cellular_componentdendrite
A0030594molecular_functionneurotransmitter receptor activity
A0045202cellular_componentsynapse
A0045907biological_processpositive regulation of vasoconstriction
B0002862biological_processnegative regulation of inflammatory response to antigenic stimulus
B0003091biological_processrenal water homeostasis
B0003924molecular_functionGTPase activity
B0003925molecular_functionG protein activity
B0005515molecular_functionprotein binding
B0005525molecular_functionGTP binding
B0005737cellular_componentcytoplasm
B0005829cellular_componentcytosol
B0005834cellular_componentheterotrimeric G-protein complex
B0005886cellular_componentplasma membrane
B0007165biological_processsignal transduction
B0007186biological_processG protein-coupled receptor signaling pathway
B0007189biological_processadenylate cyclase-activating G protein-coupled receptor signaling pathway
B0007190biological_processactivation of adenylate cyclase activity
B0007191biological_processadenylate cyclase-activating dopamine receptor signaling pathway
B0007608biological_processsensory perception of smell
B0010856molecular_functionadenylate cyclase activator activity
B0016020cellular_componentmembrane
B0016787molecular_functionhydrolase activity
B0019001molecular_functionguanyl nucleotide binding
B0031683molecular_functionG-protein beta/gamma-subunit complex binding
B0031748molecular_functionD1 dopamine receptor binding
B0032588cellular_componenttrans-Golgi network membrane
B0046872molecular_functionmetal ion binding
B0046907biological_processintracellular transport
B0048589biological_processdevelopmental growth
B0050796biological_processregulation of insulin secretion
B0050890biological_processcognition
B0060348biological_processbone development
B0060789biological_processhair follicle placode formation
B0070062cellular_componentextracellular exosome
B0070527biological_processplatelet aggregation
B0071377biological_processcellular response to glucagon stimulus
B0071380biological_processcellular response to prostaglandin E stimulus
B0071870biological_processcellular response to catecholamine stimulus
B0071880biological_processadenylate cyclase-activating adrenergic receptor signaling pathway
B0120162biological_processpositive regulation of cold-induced thermogenesis
C0001750cellular_componentphotoreceptor outer segment
C0003924molecular_functionGTPase activity
C0005515molecular_functionprotein binding
C0005737cellular_componentcytoplasm
C0005765cellular_componentlysosomal membrane
C0005829cellular_componentcytosol
C0005834cellular_componentheterotrimeric G-protein complex
C0005886cellular_componentplasma membrane
C0007165biological_processsignal transduction
C0007186biological_processG protein-coupled receptor signaling pathway
C0007191biological_processadenylate cyclase-activating dopamine receptor signaling pathway
C0007200biological_processphospholipase C-activating G protein-coupled receptor signaling pathway
C0007213biological_processG protein-coupled acetylcholine receptor signaling pathway
C0007265biological_processRas protein signal transduction
C0008283biological_processcell population proliferation
C0016020cellular_componentmembrane
C0030159molecular_functionsignaling receptor complex adaptor activity
C0044877molecular_functionprotein-containing complex binding
C0045202cellular_componentsynapse
C0050909biological_processsensory perception of taste
C0051020molecular_functionGTPase binding
C0060041biological_processretina development in camera-type eye
C0070062cellular_componentextracellular exosome
C0071380biological_processcellular response to prostaglandin E stimulus
C0071870biological_processcellular response to catecholamine stimulus
C0097381cellular_componentphotoreceptor disc membrane
C1903561cellular_componentextracellular vesicle
D0005515molecular_functionprotein binding
D0005834cellular_componentheterotrimeric G-protein complex
D0005886cellular_componentplasma membrane
D0007165biological_processsignal transduction
D0007186biological_processG protein-coupled receptor signaling pathway
D0007191biological_processadenylate cyclase-activating dopamine receptor signaling pathway
D0016020cellular_componentmembrane
D0031681molecular_functionG-protein beta-subunit binding
D0045202cellular_componentsynapse
D0048144biological_processfibroblast proliferation
D0070062cellular_componentextracellular exosome
D0071380biological_processcellular response to prostaglandin E stimulus
D0071870biological_processcellular response to catecholamine stimulus
Functional Information from PROSITE/UniProt
site_idPS00237
Number of Residues17
DetailsG_PROTEIN_RECEP_F1_1 G-protein coupled receptors family 1 signature. ASIlNLFMISLDRYCaV
ChainResidueDetails
AALA110-VAL126

site_idPS00678
Number of Residues15
DetailsWD_REPEATS_1 Trp-Asp (WD) repeats signature. LVSAsqDgKLIIWDS
ChainResidueDetails
CLEU75-SER89
CILE162-ILE176
CLEU290-ALA304

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues1
DetailsMOD_RES: N-acetylalanine => ECO:0007744|PubMed:19413330, ECO:0007744|PubMed:22814378
ChainResidueDetails
DALA2
BSER54
BLYS197
BASN204
BCYS223
BSER292
BARG366

site_idSWS_FT_FI2
Number of Residues1
DetailsMOD_RES: Cysteine methyl ester => ECO:0000250|UniProtKB:P63212
ChainResidueDetails
DCYS68

site_idSWS_FT_FI3
Number of Residues1
DetailsLIPID: S-geranylgeranyl cysteine => ECO:0000250|UniProtKB:P63212
ChainResidueDetails
DCYS68
AASP121-ARG140
AILE211-VAL240
AALA296-ARG365

site_idSWS_FT_FI4
Number of Residues1
DetailsLIPID: N-palmitoyl glycine => ECO:0000250|UniProtKB:P04896
ChainResidueDetails
BGLY2

site_idSWS_FT_FI5
Number of Residues1
DetailsLIPID: S-palmitoyl cysteine => ECO:0000269|PubMed:21044946
ChainResidueDetails
BCYS3

site_idSWS_FT_FI6
Number of Residues2
DetailsCROSSLNK: Glycyl lysine isopeptide (Lys-Gly) (interchain with G-Cter in ubiquitin)
ChainResidueDetails
BGLU300

site_idSWS_FT_FI7
Number of Residues23
DetailsTRANSMEM: Helical; Name=5 => ECO:0000255
ChainResidueDetails
AVAL187-ARG210

site_idSWS_FT_FI8
Number of Residues23
DetailsTRANSMEM: Helical; Name=6 => ECO:0000255
ChainResidueDetails
ATHR241-GLY264

site_idSWS_FT_FI9
Number of Residues21
DetailsTRANSMEM: Helical; Name=7 => ECO:0000255
ChainResidueDetails
AVAL274-ALA295

site_idSWS_FT_FI10
Number of Residues1
DetailsSITE: Essential for histamine binding => ECO:0000250
ChainResidueDetails
AASP104

site_idSWS_FT_FI11
Number of Residues1
DetailsSITE: Essential for tiotidine binding and implicated in H2 selectivity => ECO:0000250
ChainResidueDetails
AASP192

site_idSWS_FT_FI12
Number of Residues1
DetailsSITE: Implicated in histamine binding => ECO:0000250
ChainResidueDetails
ATHR196

site_idSWS_FT_FI13
Number of Residues1
DetailsLIPID: S-palmitoyl cysteine => ECO:0000250
ChainResidueDetails
ACYS311

site_idSWS_FT_FI14
Number of Residues1
DetailsCARBOHYD: N-linked (GlcNAc...) asparagine => ECO:0000255
ChainResidueDetails
AASN10

227111

PDB entries from 2024-11-06

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