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4MQU

Human GKRP complexed to AMG-3969 and S6P

Functional Information from GO Data
ChainGOidnamespacecontents
A0001678biological_processintracellular glucose homeostasis
A0005515molecular_functionprotein binding
A0005634cellular_componentnucleus
A0005654cellular_componentnucleoplasm
A0005737cellular_componentcytoplasm
A0005739cellular_componentmitochondrion
A0005829cellular_componentcytosol
A0006606biological_processprotein import into nucleus
A0009749biological_processresponse to glucose
A0009750biological_processresponse to fructose
A0019210molecular_functionkinase inhibitor activity
A0033132biological_processnegative regulation of glucokinase activity
A0034504biological_processprotein localization to nucleus
A0046415biological_processurate metabolic process
A0070095molecular_functionfructose-6-phosphate binding
A0070328biological_processtriglyceride homeostasis
A0097367molecular_functioncarbohydrate derivative binding
A0141089molecular_functionglucose sensor activity
A1901135biological_processcarbohydrate derivative metabolic process
B0001678biological_processintracellular glucose homeostasis
B0005515molecular_functionprotein binding
B0005634cellular_componentnucleus
B0005654cellular_componentnucleoplasm
B0005737cellular_componentcytoplasm
B0005739cellular_componentmitochondrion
B0005829cellular_componentcytosol
B0006606biological_processprotein import into nucleus
B0009749biological_processresponse to glucose
B0009750biological_processresponse to fructose
B0019210molecular_functionkinase inhibitor activity
B0033132biological_processnegative regulation of glucokinase activity
B0034504biological_processprotein localization to nucleus
B0046415biological_processurate metabolic process
B0070095molecular_functionfructose-6-phosphate binding
B0070328biological_processtriglyceride homeostasis
B0097367molecular_functioncarbohydrate derivative binding
B0141089molecular_functionglucose sensor activity
B1901135biological_processcarbohydrate derivative metabolic process
Functional Information from PDB Data
site_idAC1
Number of Residues18
DetailsBINDING SITE FOR RESIDUE MG9 A 701
ChainResidue
AVAL28
AHIS504
ALYS514
ATRP517
AALA521
AMET522
AARG525
AIOD710
AHOH801
AHOH890
APRO29
AGLU32
ASER34
AGLY181
AASN209
AMET213
AARG215
AASP217

site_idAC2
Number of Residues22
DetailsBINDING SITE FOR RESIDUE S6P A 702
ChainResidue
AGLY107
AGLY108
ATHR109
ASER110
AGLU150
AGLU153
ASER179
AVAL180
AGLY181
AALA184
ASER257
ASER258
AARG259
AHIS351
ALYS514
AHOH835
AHOH836
AHOH852
AHOH859
AHOH874
AHOH884
AHOH885

site_idAC3
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD A 703
ChainResidue
APHE472

site_idAC4
Number of Residues2
DetailsBINDING SITE FOR RESIDUE IOD A 705
ChainResidue
AARG73
AGLY250

site_idAC5
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD A 706
ChainResidue
AALA46

site_idAC6
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD A 707
ChainResidue
ATHR298

site_idAC7
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD A 708
ChainResidue
AGLY151

site_idAC8
Number of Residues2
DetailsBINDING SITE FOR RESIDUE IOD A 709
ChainResidue
AGLY3
ALYS5

site_idAC9
Number of Residues3
DetailsBINDING SITE FOR RESIDUE IOD A 710
ChainResidue
AGLU25
ALYS33
AMG9701

site_idBC1
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD A 711
ChainResidue
ALYS531

site_idBC2
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD A 712
ChainResidue
AASN196

site_idBC3
Number of Residues2
DetailsBINDING SITE FOR RESIDUE IOD A 713
ChainResidue
AGLN529
ASER530

site_idBC4
Number of Residues17
DetailsBINDING SITE FOR RESIDUE MG9 B 701
ChainResidue
BVAL28
BPRO29
BGLU32
BSER34
BGLY181
BMET213
BARG215
BASP217
BHIS504
BLYS514
BTRP517
BALA521
BMET522
BARG525
BIOD711
BHOH801
BHOH934

site_idBC5
Number of Residues21
DetailsBINDING SITE FOR RESIDUE S6P B 702
ChainResidue
BGLY107
BTHR109
BSER110
BGLU150
BGLU153
BSER179
BVAL180
BGLY181
BALA184
BSER257
BSER258
BARG259
BHIS351
BLYS514
BHOH853
BHOH855
BHOH886
BHOH892
BHOH901
BHOH913
BHOH916

site_idBC6
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD B 703
ChainResidue
BPHE472

site_idBC7
Number of Residues2
DetailsBINDING SITE FOR RESIDUE IOD B 705
ChainResidue
BARG73
BGLY250

site_idBC8
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD B 706
ChainResidue
BTHR298

site_idBC9
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD B 707
ChainResidue
BALA46

site_idCC1
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD B 708
ChainResidue
BGLY151

site_idCC2
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD B 709
ChainResidue
BSER530

site_idCC3
Number of Residues3
DetailsBINDING SITE FOR RESIDUE IOD B 710
ChainResidue
BGLY3
BLYS5
BALA554

site_idCC4
Number of Residues4
DetailsBINDING SITE FOR RESIDUE IOD B 711
ChainResidue
BGLU25
BLYS33
BSER34
BMG9701

site_idCC5
Number of Residues2
DetailsBINDING SITE FOR RESIDUE IOD B 713
ChainResidue
BLEU445
BSER458

site_idCC6
Number of Residues1
DetailsBINDING SITE FOR RESIDUE IOD B 714
ChainResidue
BASN196

site_idCC7
Number of Residues7
DetailsBINDING SITE FOR RESIDUE GOL B 716
ChainResidue
BGLY354
BASP507
BARG509
BLYS567
BGLU568
BGLN569
BHOH808

site_idCC8
Number of Residues2
DetailsBINDING SITE FOR RESIDUE SO4 B 717
ChainResidue
BALA44
BASP45

site_idCC9
Number of Residues4
DetailsBINDING SITE FOR RESIDUE SO4 B 718
ChainResidue
BLYS18
BLEU21
BSER22
BHOH852

site_idDC1
Number of Residues3
DetailsBINDING SITE FOR RESIDUE SO4 B 719
ChainResidue
BGLN336
BTHR337
BLEU364

Functional Information from PROSITE/UniProt
site_idPS01272
Number of Residues18
DetailsGCKR Glucokinase regulatory protein family signature. GPEgLSGSSRMKGGSatK
ChainResidueDetails
AGLY250-LYS267

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues392
DetailsDomain: {"description":"SIS 1","evidences":[{"source":"PROSITE-ProRule","id":"PRU00797","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI2
Number of Residues2
DetailsRegion: {"description":"Important for interaction with GCK","evidences":[{"source":"UniProtKB","id":"Q07071","evidenceCode":"ECO:0000250"}]}
ChainResidueDetails

site_idSWS_FT_FI3
Number of Residues4
DetailsRegion: {"description":"Essential for interaction with GCK","evidences":[{"source":"PubMed","id":"23733961","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI4
Number of Residues8
DetailsBinding site: {"evidences":[{"source":"UniProtKB","id":"Q07071","evidenceCode":"ECO:0000250"}]}
ChainResidueDetails

site_idSWS_FT_FI5
Number of Residues4
DetailsBinding site: {"evidences":[{"source":"PubMed","id":"23621087","evidenceCode":"ECO:0000269"},{"source":"PDB","id":"4BB9","evidenceCode":"ECO:0007744"}]}
ChainResidueDetails

238895

PDB entries from 2025-07-16

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