Structure of PDB 6o2p Chain A
Receptor sequence
>6o2pA (length=1179) Species:
9606
(Homo sapiens) [
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MQRSPLEKASVVSKLFFSWTRPILRKGYRQRLELSDIYQIPSVDSADNLS
EKLEREWDRELASKKNPKLINALRRCFFWRFMFYGIFLYLGEVTKAVQPL
LLGRIIASYDPDNKEERSIAIYLGIGLCLLFIVRTLLLHPAIFGLHHIGM
QMRIAMFSLIYKKTLKLSSRVLDKISIGQLVSLLSNNLNKFDEGLALAHF
VWIAPLQVALLMGLIWELLQASAFCGLGFLIVLALFQAGLGRMMMKYRDQ
RAGKISERLVITSEMIENIQSVKAYCWEEAMEKMIENLRQTELKLTRKAA
YVRYFNSSAFFFSGFFVVFLSVLPYALIKGIILRKIFTTISFCIVLRMAV
TRQFPWAVQTWYDSLGAINKIQDFLQKQEYKTLEYNLTTTEVVMENVTAF
WEEGFGELFGTPVLKDINFKIERGQLLAVAGSTGAGKTSLLMVIMGELEP
SEGKIKHSGRISFCSQFSWIMPGTIKENIIFGVSYDEYRYRSVIKACQLE
EDISKFAEKDNIVLGEGGITLSGGQRARISLARAVYKDADLYLLDSPFGY
LDVLTEKEIFESCVCKLMANKTRILVTSKMEHLKKADKILILHEGSSYFY
GTFSELQNLQTWNTYLRYITVHKSLIFVLIWCLVIFLAEVAASLVVLWLL
GNTPLNNSYAVIITSTSSYYVFYIYVGVADTLLAMGFFRGLPLVHTLITV
SKILHHKMLHSVLQAPMSTLNTLKAGGILNRFSKDIAILDDLLPLTIFDF
IQLLLIVIGAIAVVAVLQPYIFVATVPVIVAFIMLRAYFLQTSQQLKQLE
SEGRSPIFTHLVTSLKGLWTLRAFGRQPYFETLFHKALNLHTANWFLYLS
TLRWFQMRIEMIFVIFFIAVTFISILTTGEGEGRVGIILTLAMNIMSTLQ
WAVNSSIDVDSLMRSVSRVFKFIDMPTEGDIWPSGGQMTVKDLTAKYTEG
GNAILENISFSISPGQRVGLLGRTGSGKSTLLSAFLRLLNTEGEIQIDGV
SWDSITLQQWRKAFGVIPQKVFIFSGTFRKNLDPYEQWSDQEIWKVADEV
GLRSVIEQFPGKLDFVLVDGGCVLSHGHKQLMCLARSVLSKAKILLLDQP
SAHLDPVTYQIIRRTLKQAFADCTVILCEHRIEAMLECQQFLVIEENKVR
QYDSIQKLLNERSLFRQAISPSDRVKLFP
3D structure
PDB
6o2p
Structural identification of a hotspot on CFTR for potentiation.
Chain
A
Resolution
3.3 Å
3D
structure
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Enzymatic activity
Enzyme Commision number
5.6.1.6
: channel-conductance-controlling ATPase.
Interaction with ligand
Site
#
Ligand
Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01
peptide
A
M1 L34 E1046 L1084
M1 L34 E802 L840
BS02
MG
A
T465 Q493
T438 Q466
BS03
MG
A
S1251 Q1291
S979 Q1019
BS04
ATP
A
W401 V440 G461 G463 K464 T465 S466 Q493 V1345 S1347 H1348 G1349
W401 V413 G434 G436 K437 T438 S439 Q466 V1073 S1075 H1076 G1077
BS05
ATP
A
F533 T547 S549 G550 G551 Q552 Y1219 T1246 G1247 G1249 K1250 S1251 T1252 Q1291
F506 T520 S522 G523 G524 Q525 Y947 T974 G975 G977 K978 S979 T980 Q1019
BS06
VX7
A
F305 A309 F312 F931 F932
F305 A309 F312 F687 F688
PDBbind-CN
: -logKd/Ki=8.18,Kd=6.6nM
BindingDB: EC50=236nM
Gene Ontology
Molecular Function
GO:0005254
chloride channel activity
GO:0005260
intracellularly ATP-gated chloride channel activity
GO:0005515
protein binding
GO:0005524
ATP binding
GO:0015106
bicarbonate transmembrane transporter activity
GO:0015108
chloride transmembrane transporter activity
GO:0016853
isomerase activity
GO:0016887
ATP hydrolysis activity
GO:0017081
chloride channel regulator activity
GO:0019869
chloride channel inhibitor activity
GO:0019899
enzyme binding
GO:0030165
PDZ domain binding
GO:0042626
ATPase-coupled transmembrane transporter activity
GO:0043225
ATPase-coupled inorganic anion transmembrane transporter activity
GO:0051087
protein-folding chaperone binding
GO:0071889
14-3-3 protein binding
GO:0106138
Sec61 translocon complex binding
GO:0140359
ABC-type transporter activity
Biological Process
GO:0006695
cholesterol biosynthetic process
GO:0006811
monoatomic ion transport
GO:0006821
chloride transport
GO:0006904
vesicle docking involved in exocytosis
GO:0015701
bicarbonate transport
GO:0030301
cholesterol transport
GO:0034220
monoatomic ion transmembrane transport
GO:0034976
response to endoplasmic reticulum stress
GO:0035377
transepithelial water transport
GO:0035774
positive regulation of insulin secretion involved in cellular response to glucose stimulus
GO:0045921
positive regulation of exocytosis
GO:0048240
sperm capacitation
GO:0050891
multicellular organismal-level water homeostasis
GO:0051454
intracellular pH elevation
GO:0051649
establishment of localization in cell
GO:0055085
transmembrane transport
GO:0060081
membrane hyperpolarization
GO:0070175
positive regulation of enamel mineralization
GO:0071320
cellular response to cAMP
GO:0097186
amelogenesis
GO:1902161
positive regulation of cyclic nucleotide-gated ion channel activity
GO:1902476
chloride transmembrane transport
GO:1902943
positive regulation of voltage-gated chloride channel activity
GO:1904322
cellular response to forskolin
Cellular Component
GO:0005634
nucleus
GO:0005737
cytoplasm
GO:0005765
lysosomal membrane
GO:0005768
endosome
GO:0005769
early endosome
GO:0005783
endoplasmic reticulum
GO:0005789
endoplasmic reticulum membrane
GO:0005829
cytosol
GO:0005886
plasma membrane
GO:0009986
cell surface
GO:0010008
endosome membrane
GO:0016020
membrane
GO:0016324
apical plasma membrane
GO:0030660
Golgi-associated vesicle membrane
GO:0030669
clathrin-coated endocytic vesicle membrane
GO:0031901
early endosome membrane
GO:0032991
protein-containing complex
GO:0034707
chloride channel complex
GO:0055037
recycling endosome
GO:0055038
recycling endosome membrane
View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB
RCSB:6o2p
,
PDBe:6o2p
,
PDBj:6o2p
PDBsum
6o2p
PubMed
31221859
UniProt
P13569
|CFTR_HUMAN Cystic fibrosis transmembrane conductance regulator (Gene Name=CFTR)
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