6UR8

CryoEM structure of human alpha4beta2 nicotinic acetylcholine receptor in complex with varenicline

Functional Information from GO Data

Chain	GOid	namespace	contents
A	0004888	molecular_function	transmembrane signaling receptor activity
A	0005216	molecular_function	monoatomic ion channel activity
A	0005230	molecular_function	extracellular ligand-gated monoatomic ion channel activity
A	0005506	molecular_function	iron ion binding
A	0006811	biological_process	monoatomic ion transport
A	0009055	molecular_function	electron transfer activity
A	0016020	cellular_component	membrane
A	0020037	molecular_function	heme binding
A	0022848	molecular_function	acetylcholine-gated monoatomic cation-selective channel activity
A	0022900	biological_process	electron transport chain
A	0034220	biological_process	monoatomic ion transmembrane transport
A	0042597	cellular_component	periplasmic space
A	0045211	cellular_component	postsynaptic membrane
A	0046872	molecular_function	metal ion binding
B	0004888	molecular_function	transmembrane signaling receptor activity
B	0005216	molecular_function	monoatomic ion channel activity
B	0005230	molecular_function	extracellular ligand-gated monoatomic ion channel activity
B	0006811	biological_process	monoatomic ion transport
B	0016020	cellular_component	membrane
B	0022848	molecular_function	acetylcholine-gated monoatomic cation-selective channel activity
B	0034220	biological_process	monoatomic ion transmembrane transport
B	0045211	cellular_component	postsynaptic membrane
C	0004888	molecular_function	transmembrane signaling receptor activity
C	0005216	molecular_function	monoatomic ion channel activity
C	0005230	molecular_function	extracellular ligand-gated monoatomic ion channel activity
C	0006811	biological_process	monoatomic ion transport
C	0016020	cellular_component	membrane
C	0022848	molecular_function	acetylcholine-gated monoatomic cation-selective channel activity
C	0034220	biological_process	monoatomic ion transmembrane transport
C	0045211	cellular_component	postsynaptic membrane
D	0004888	molecular_function	transmembrane signaling receptor activity
D	0005216	molecular_function	monoatomic ion channel activity
D	0005230	molecular_function	extracellular ligand-gated monoatomic ion channel activity
D	0005506	molecular_function	iron ion binding
D	0006811	biological_process	monoatomic ion transport
D	0009055	molecular_function	electron transfer activity
D	0016020	cellular_component	membrane
D	0020037	molecular_function	heme binding
D	0022848	molecular_function	acetylcholine-gated monoatomic cation-selective channel activity
D	0022900	biological_process	electron transport chain
D	0034220	biological_process	monoatomic ion transmembrane transport
D	0042597	cellular_component	periplasmic space
D	0045211	cellular_component	postsynaptic membrane
D	0046872	molecular_function	metal ion binding
E	0004888	molecular_function	transmembrane signaling receptor activity
E	0005216	molecular_function	monoatomic ion channel activity
E	0005230	molecular_function	extracellular ligand-gated monoatomic ion channel activity
E	0006811	biological_process	monoatomic ion transport
E	0016020	cellular_component	membrane
E	0022848	molecular_function	acetylcholine-gated monoatomic cation-selective channel activity
E	0034220	biological_process	monoatomic ion transmembrane transport
E	0045211	cellular_component	postsynaptic membrane

Functional Information from PROSITE/UniProt

site_id	PS00236
Number of Residues	15
Details	NEUROTR_ION_CHANNEL Neurotransmitter-gated ion-channels signature. CsIdVtfFPfDqqnC

Chain	Residue	Details
A	CYS135-CYS149
B	CYS130-CYS144

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Functional Information from SwissProt/UniProt

site_id	SWS_FT_FI1
Number of Residues	663
Details	TOPO_DOM: Extracellular => ECO:0000255

Chain	Residue	Details
B	THR1-LYS208
B	LYS260-LYS274
C	THR1-LYS208
C	LYS260-LYS274
E	THR1-LYS208
E	LYS260-LYS274

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site_id	SWS_FT_FI2
Number of Residues	246
Details	TRANSMEM: Helical => ECO:0000255

Chain	Residue	Details
B	PRO209-LEU233
E	MET241-SER259
E	TYR275-VAL296
E	ASP346-PHE365
B	MET241-SER259
B	TYR275-VAL296
B	ASP346-PHE365
C	PRO209-LEU233
C	MET241-SER259
C	TYR275-VAL296
C	ASP346-PHE365
E	PRO209-LEU233

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site_id	SWS_FT_FI3
Number of Residues	426
Details	TOPO_DOM: Cytoplasmic => ECO:0000255

Chain	Residue	Details
B	PRO234-LYS240
D	CYS245
C	PRO234-LYS240
E	PRO234-LYS240

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site_id	SWS_FT_FI4
Number of Residues	3
Details	SITE: Key residue that may interfere with effective access of the conotoxin BuIA to the channel binding site => ECO:0000250|UniProtKB:P12390

Chain	Residue	Details
B	THR59
C	THR59
E	THR59
D	ASN31
D	ASN81
D	ASN148

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site_id	SWS_FT_FI5
Number of Residues	6
Details	SITE: Key residue for a rapid dissociation (K(off)) from the conotoxin BuIA => ECO:0000250|UniProtKB:P12390

Chain	Residue	Details
B	VAL111
B	PHE119
C	VAL111
C	PHE119
E	VAL111
E	PHE119

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site_id	SWS_FT_FI6
Number of Residues	9
Details	CARBOHYD: N-linked (GlcNAc...) asparagine => ECO:0000255

Chain	Residue	Details
B	ASN26
B	ASN143
B	ASN372
C	ASN26
C	ASN143
C	ASN372
E	ASN26
E	ASN143
E	ASN372

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