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3G5U

Structure of P-glycoprotein Reveals a Molecular Basis for Poly-Specific Drug Binding

Functional Information from GO Data
ChainGOidnamespacecontents
A0000086biological_processG2/M transition of mitotic cell cycle
A0005524molecular_functionATP binding
A0005737cellular_componentcytoplasm
A0005886cellular_componentplasma membrane
A0007173biological_processepidermal growth factor receptor signaling pathway
A0007507biological_processheart development
A0007512biological_processadult heart development
A0008559molecular_functionABC-type xenobiotic transporter activity
A0008585biological_processfemale gonad development
A0009410biological_processresponse to xenobiotic stimulus
A0009636biological_processresponse to toxic substance
A0009986cellular_componentcell surface
A0010467biological_processgene expression
A0010498biological_processproteasomal protein catabolic process
A0015562molecular_functionefflux transmembrane transporter activity
A0016020cellular_componentmembrane
A0016324cellular_componentapical plasma membrane
A0016887molecular_functionATP hydrolysis activity
A0022008biological_processneurogenesis
A0022857molecular_functiontransmembrane transporter activity
A0031625molecular_functionubiquitin protein ligase binding
A0035640biological_processexploration behavior
A0035932biological_processaldosterone secretion
A0042626molecular_functionATPase-coupled transmembrane transporter activity
A0042908biological_processxenobiotic transport
A0042910molecular_functionxenobiotic transmembrane transporter activity
A0045332biological_processphospholipid translocation
A0046581cellular_componentintercellular canaliculus
A0046865biological_processterpenoid transport
A0046943molecular_functioncarboxylic acid transmembrane transporter activity
A0055007biological_processcardiac muscle cell differentiation
A0055085biological_processtransmembrane transport
A0070633biological_processtransepithelial transport
A0072089biological_processstem cell proliferation
A0090554molecular_functionphosphatidylcholine floppase activity
A0090555molecular_functionphosphatidylethanolamine flippase activity
A0097719biological_processneural tissue regeneration
A0099038molecular_functionceramide floppase activity
A0099040biological_processceramide translocation
A0140115biological_processexport across plasma membrane
A0140326molecular_functionATPase-coupled intramembrane lipid transporter activity
A0140328molecular_functionfloppase activity
A0140341molecular_functionphosphatidylethanolamine floppase activity
A0140359molecular_functionABC-type transporter activity
A1905039biological_processcarboxylic acid transmembrane transport
A1990961biological_processxenobiotic detoxification by transmembrane export across the plasma membrane
A1990962biological_processxenobiotic transport across blood-brain barrier
A2001225biological_processregulation of chloride transport
B0000086biological_processG2/M transition of mitotic cell cycle
B0005524molecular_functionATP binding
B0005737cellular_componentcytoplasm
B0005886cellular_componentplasma membrane
B0007173biological_processepidermal growth factor receptor signaling pathway
B0007507biological_processheart development
B0007512biological_processadult heart development
B0008559molecular_functionABC-type xenobiotic transporter activity
B0008585biological_processfemale gonad development
B0009410biological_processresponse to xenobiotic stimulus
B0009636biological_processresponse to toxic substance
B0009986cellular_componentcell surface
B0010467biological_processgene expression
B0010498biological_processproteasomal protein catabolic process
B0015562molecular_functionefflux transmembrane transporter activity
B0016020cellular_componentmembrane
B0016324cellular_componentapical plasma membrane
B0016887molecular_functionATP hydrolysis activity
B0022008biological_processneurogenesis
B0022857molecular_functiontransmembrane transporter activity
B0031625molecular_functionubiquitin protein ligase binding
B0035640biological_processexploration behavior
B0035932biological_processaldosterone secretion
B0042626molecular_functionATPase-coupled transmembrane transporter activity
B0042908biological_processxenobiotic transport
B0042910molecular_functionxenobiotic transmembrane transporter activity
B0045332biological_processphospholipid translocation
B0046581cellular_componentintercellular canaliculus
B0046865biological_processterpenoid transport
B0046943molecular_functioncarboxylic acid transmembrane transporter activity
B0055007biological_processcardiac muscle cell differentiation
B0055085biological_processtransmembrane transport
B0070633biological_processtransepithelial transport
B0072089biological_processstem cell proliferation
B0090554molecular_functionphosphatidylcholine floppase activity
B0090555molecular_functionphosphatidylethanolamine flippase activity
B0097719biological_processneural tissue regeneration
B0099038molecular_functionceramide floppase activity
B0099040biological_processceramide translocation
B0140115biological_processexport across plasma membrane
B0140326molecular_functionATPase-coupled intramembrane lipid transporter activity
B0140328molecular_functionfloppase activity
B0140341molecular_functionphosphatidylethanolamine floppase activity
B0140359molecular_functionABC-type transporter activity
B1905039biological_processcarboxylic acid transmembrane transport
B1990961biological_processxenobiotic detoxification by transmembrane export across the plasma membrane
B1990962biological_processxenobiotic transport across blood-brain barrier
B2001225biological_processregulation of chloride transport
Functional Information from PDB Data
site_idAC1
Number of Residues2
DetailsBINDING SITE FOR RESIDUE HG A1285
ChainResidue
ATRP132
ACYS133

site_idAC2
Number of Residues2
DetailsBINDING SITE FOR RESIDUE HG A1286
ChainResidue
ATYR397
ACYS427

site_idAC3
Number of Residues3
DetailsBINDING SITE FOR RESIDUE HG A1287
ChainResidue
ACYS713
AALA714
AGLN769

site_idAC4
Number of Residues1
DetailsBINDING SITE FOR RESIDUE HG A1288
ChainResidue
ACYS1070

site_idAC5
Number of Residues2
DetailsBINDING SITE FOR RESIDUE HG A1289
ChainResidue
ACYS1121
APHE1119

site_idAC6
Number of Residues4
DetailsBINDING SITE FOR RESIDUE HG A1290
ChainResidue
ATHR1061
ALEU1195
ACYS1223
AVAL1225

site_idAC7
Number of Residues2
DetailsBINDING SITE FOR RESIDUE HG B1285
ChainResidue
BTRP132
BCYS133

site_idAC8
Number of Residues1
DetailsBINDING SITE FOR RESIDUE HG B1286
ChainResidue
BCYS427

site_idAC9
Number of Residues3
DetailsBINDING SITE FOR RESIDUE HG B1287
ChainResidue
BCYS713
BALA714
BGLN769

site_idBC1
Number of Residues1
DetailsBINDING SITE FOR RESIDUE HG B1288
ChainResidue
BCYS1070

site_idBC2
Number of Residues2
DetailsBINDING SITE FOR RESIDUE HG B1289
ChainResidue
BPHE1119
BCYS1121

site_idBC3
Number of Residues5
DetailsBINDING SITE FOR RESIDUE HG B1290
ChainResidue
BLEU1195
BLEU1214
BARG1218
BCYS1223
BVAL1225

Functional Information from PROSITE/UniProt
site_idPS00211
Number of Residues15
DetailsABC_TRANSPORTER_1 ABC transporters family signature. LSGGQKQRIAIARAL
ChainResidueDetails
ALEU527-LEU541
ALEU1172-LEU1186

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues494
DetailsTransmembrane: {"description":"Helical"}
ChainResidueDetails

site_idSWS_FT_FI2
Number of Residues206
DetailsTopological domain: {"description":"Extracellular","evidences":[{"evidenceCode":"ECO:0000250"}]}
ChainResidueDetails

site_idSWS_FT_FI3
Number of Residues436
DetailsTopological domain: {"description":"Cytoplasmic","evidences":[{"evidenceCode":"ECO:0000250"}]}
ChainResidueDetails

site_idSWS_FT_FI4
Number of Residues606
DetailsDomain: {"description":"ABC transmembrane type-1 1","evidences":[{"source":"PROSITE-ProRule","id":"PRU00441","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI5
Number of Residues472
DetailsDomain: {"description":"ABC transporter 1","evidences":[{"source":"PROSITE-ProRule","id":"PRU00434","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI6
Number of Residues578
DetailsDomain: {"description":"ABC transmembrane type-1 2","evidences":[{"source":"PROSITE-ProRule","id":"PRU00441","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI7
Number of Residues476
DetailsDomain: {"description":"ABC transporter 2","evidences":[{"source":"PROSITE-ProRule","id":"PRU00434","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI8
Number of Residues28
DetailsBinding site: {"evidences":[{"source":"PROSITE-ProRule","id":"PRU00434","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI9
Number of Residues6
DetailsGlycosylation: {"description":"N-linked (GlcNAc...) asparagine","evidences":[{"evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

251174

PDB entries from 2026-03-25

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