4PXS
Human GKRP bound to AMG-0265 (N-[(R)-(2-CHLOROPHENYL){7-[4-(2-HYDROXYPROPAN-2-YL) PYRIDIN-2-YL]-1-BENZOTHIOPHEN-2-YL}METHYL]CYCLOPROPANESULFONAMIDE) and Sorbitol-6-phosphate
Functional Information from GO Data
Chain | GOid | namespace | contents |
A | 0004857 | molecular_function | enzyme inhibitor activity |
A | 0005515 | molecular_function | protein binding |
A | 0005634 | cellular_component | nucleus |
A | 0005654 | cellular_component | nucleoplasm |
A | 0005737 | cellular_component | cytoplasm |
A | 0005739 | cellular_component | mitochondrion |
A | 0005829 | cellular_component | cytosol |
A | 0006606 | biological_process | protein import into nucleus |
A | 0009749 | biological_process | response to glucose |
A | 0009750 | biological_process | response to fructose |
A | 0019210 | molecular_function | kinase inhibitor activity |
A | 0019899 | molecular_function | enzyme binding |
A | 0030246 | molecular_function | carbohydrate binding |
A | 0033132 | biological_process | negative regulation of glucokinase activity |
A | 0042593 | biological_process | glucose homeostasis |
A | 0046415 | biological_process | urate metabolic process |
A | 0070095 | molecular_function | fructose-6-phosphate binding |
A | 0070328 | biological_process | triglyceride homeostasis |
A | 0097367 | molecular_function | carbohydrate derivative binding |
A | 0141089 | molecular_function | glucose sensor activity |
A | 1901135 | biological_process | carbohydrate derivative metabolic process |
B | 0004857 | molecular_function | enzyme inhibitor activity |
B | 0005515 | molecular_function | protein binding |
B | 0005634 | cellular_component | nucleus |
B | 0005654 | cellular_component | nucleoplasm |
B | 0005737 | cellular_component | cytoplasm |
B | 0005739 | cellular_component | mitochondrion |
B | 0005829 | cellular_component | cytosol |
B | 0006606 | biological_process | protein import into nucleus |
B | 0009749 | biological_process | response to glucose |
B | 0009750 | biological_process | response to fructose |
B | 0019210 | molecular_function | kinase inhibitor activity |
B | 0019899 | molecular_function | enzyme binding |
B | 0030246 | molecular_function | carbohydrate binding |
B | 0033132 | biological_process | negative regulation of glucokinase activity |
B | 0042593 | biological_process | glucose homeostasis |
B | 0046415 | biological_process | urate metabolic process |
B | 0070095 | molecular_function | fructose-6-phosphate binding |
B | 0070328 | biological_process | triglyceride homeostasis |
B | 0097367 | molecular_function | carbohydrate derivative binding |
B | 0141089 | molecular_function | glucose sensor activity |
B | 1901135 | biological_process | carbohydrate derivative metabolic process |
Functional Information from PDB Data
site_id | AC1 |
Number of Residues | 14 |
Details | BINDING SITE FOR RESIDUE 2Y6 A 701 |
Chain | Residue |
A | HIS9 |
A | ASP217 |
A | TRP517 |
A | ALA521 |
A | ARG525 |
A | HOH833 |
A | TYR24 |
A | VAL28 |
A | PRO29 |
A | GLU32 |
A | GLY181 |
A | MET213 |
A | ARG215 |
A | ASN216 |
site_id | AC2 |
Number of Residues | 16 |
Details | BINDING SITE FOR RESIDUE S6P A 702 |
Chain | Residue |
A | GLY107 |
A | THR109 |
A | SER110 |
A | GLU150 |
A | GLU153 |
A | SER179 |
A | VAL180 |
A | GLY181 |
A | ALA184 |
A | SER257 |
A | SER258 |
A | ARG259 |
A | HIS351 |
A | LYS514 |
A | HOH813 |
A | HOH820 |
site_id | AC3 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD A 705 |
Chain | Residue |
A | ARG73 |
site_id | AC4 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD A 706 |
Chain | Residue |
A | ALA46 |
site_id | AC5 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD A 707 |
Chain | Residue |
A | THR298 |
site_id | AC6 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD A 708 |
Chain | Residue |
A | GLY151 |
site_id | AC7 |
Number of Residues | 2 |
Details | BINDING SITE FOR RESIDUE IOD A 709 |
Chain | Residue |
A | GLY3 |
A | LYS5 |
site_id | AC8 |
Number of Residues | 2 |
Details | BINDING SITE FOR RESIDUE IOD A 710 |
Chain | Residue |
A | GLU25 |
A | LYS33 |
site_id | AC9 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD A 711 |
Chain | Residue |
A | LYS531 |
site_id | BC1 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD A 712 |
Chain | Residue |
A | ASN196 |
site_id | BC2 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD A 713 |
Chain | Residue |
A | SER530 |
site_id | BC3 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD A 715 |
Chain | Residue |
A | HIS565 |
site_id | BC4 |
Number of Residues | 15 |
Details | BINDING SITE FOR RESIDUE 2Y6 B 701 |
Chain | Residue |
B | HIS9 |
B | TYR24 |
B | VAL28 |
B | PRO29 |
B | GLU32 |
B | GLY181 |
B | MET213 |
B | ARG215 |
B | ASN216 |
B | ASP217 |
B | HIS504 |
B | TRP517 |
B | ALA521 |
B | ARG525 |
B | HOH849 |
site_id | BC5 |
Number of Residues | 22 |
Details | BINDING SITE FOR RESIDUE S6P B 702 |
Chain | Residue |
B | GLY107 |
B | GLY108 |
B | THR109 |
B | SER110 |
B | GLU150 |
B | GLU153 |
B | SER179 |
B | VAL180 |
B | GLY181 |
B | ALA184 |
B | SER257 |
B | SER258 |
B | ARG259 |
B | HIS351 |
B | LYS514 |
B | HOH810 |
B | HOH811 |
B | HOH821 |
B | HOH822 |
B | HOH824 |
B | HOH828 |
B | HOH830 |
site_id | BC6 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD B 703 |
Chain | Residue |
B | PHE472 |
site_id | BC7 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD B 705 |
Chain | Residue |
B | ARG73 |
site_id | BC8 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD B 706 |
Chain | Residue |
B | THR298 |
site_id | BC9 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD B 708 |
Chain | Residue |
B | GLY151 |
site_id | CC1 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD B 709 |
Chain | Residue |
B | SER530 |
site_id | CC2 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD B 710 |
Chain | Residue |
B | GLY3 |
site_id | CC3 |
Number of Residues | 3 |
Details | BINDING SITE FOR RESIDUE IOD B 711 |
Chain | Residue |
B | GLU25 |
B | LYS33 |
B | SER34 |
site_id | CC4 |
Number of Residues | 2 |
Details | BINDING SITE FOR RESIDUE IOD B 712 |
Chain | Residue |
B | THR4 |
B | LYS531 |
site_id | CC5 |
Number of Residues | 2 |
Details | BINDING SITE FOR RESIDUE IOD B 713 |
Chain | Residue |
B | LEU445 |
B | SER458 |
site_id | CC6 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD B 715 |
Chain | Residue |
B | GLU12 |
site_id | CC7 |
Number of Residues | 3 |
Details | BINDING SITE FOR RESIDUE IOD B 716 |
Chain | Residue |
B | GLY127 |
B | LEU128 |
B | GLU469 |
site_id | CC8 |
Number of Residues | 1 |
Details | BINDING SITE FOR RESIDUE IOD B 717 |
Chain | Residue |
B | GLN502 |
site_id | CC9 |
Number of Residues | 6 |
Details | BINDING SITE FOR RESIDUE GOL B 719 |
Chain | Residue |
B | ARG509 |
B | LYS567 |
B | GLN569 |
B | HOH802 |
B | GLY354 |
B | ASP507 |
site_id | DC1 |
Number of Residues | 3 |
Details | BINDING SITE FOR RESIDUE GOL B 720 |
Chain | Residue |
B | LYS164 |
B | ALA167 |
B | PHE201 |
site_id | DC2 |
Number of Residues | 2 |
Details | BINDING SITE FOR RESIDUE SO4 B 721 |
Chain | Residue |
B | ASP42 |
B | ALA44 |
site_id | DC3 |
Number of Residues | 3 |
Details | BINDING SITE FOR RESIDUE SO4 B 722 |
Chain | Residue |
B | GLN336 |
B | THR337 |
B | LEU364 |
site_id | DC4 |
Number of Residues | 3 |
Details | BINDING SITE FOR RESIDUE SO4 B 723 |
Chain | Residue |
B | MET236 |
B | LYS239 |
B | LYS241 |
Functional Information from PROSITE/UniProt
site_id | PS01272 |
Number of Residues | 18 |
Details | GCKR Glucokinase regulatory protein family signature. GPEgLSGSSRMKGGSatK |
Chain | Residue | Details |
A | GLY250-LYS267 |
Functional Information from SwissProt/UniProt
site_id | SWS_FT_FI1 |
Number of Residues | 6 |
Details | BINDING: BINDING => ECO:0000250|UniProtKB:Q07071 |
Chain | Residue | Details |
B | SER179 | |
B | LYS514 | |
A | THR109 | |
A | SER179 | |
A | LYS514 | |
B | THR109 |
site_id | SWS_FT_FI2 |
Number of Residues | 4 |
Details | BINDING: BINDING => ECO:0000269|PubMed:23621087, ECO:0007744|PDB:4BB9 |
Chain | Residue | Details |
B | GLU153 | |
B | GLU348 | |
A | GLU153 | |
A | GLU348 |