4LY9
Human GKRP complexed to AMG-1694 [(2R)-1,1,1-trifluoro-2-{4-[(2S)-2-{[(3S)-3-methylmorpholin-4-yl]methyl}-4-(thiophen-2-ylsulfonyl)piperazin-1-yl]phenyl}propan-2-ol] 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 | 0009254 | biological_process | peptidoglycan turnover |
| A | 0009749 | biological_process | response to glucose |
| A | 0009750 | biological_process | response to fructose |
| A | 0016803 | molecular_function | ether hydrolase activity |
| A | 0016835 | molecular_function | carbon-oxygen lyase activity |
| 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 | 0046348 | biological_process | amino sugar catabolic process |
| 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 | 0009254 | biological_process | peptidoglycan turnover |
| B | 0009749 | biological_process | response to glucose |
| B | 0009750 | biological_process | response to fructose |
| B | 0016803 | molecular_function | ether hydrolase activity |
| B | 0016835 | molecular_function | carbon-oxygen lyase activity |
| 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 | 0046348 | biological_process | amino sugar catabolic process |
| 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 | 2 |
| Details | BINDING SITE FOR RESIDUE IOD A 701 |
| Chain | Residue |
| A | TYR468 |
| A | PHE472 |
| site_id | AC2 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD A 703 |
| Chain | Residue |
| A | ARG73 |
| site_id | AC3 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD A 704 |
| Chain | Residue |
| A | ALA46 |
| site_id | AC4 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD A 705 |
| Chain | Residue |
| A | THR298 |
| site_id | AC5 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD A 706 |
| Chain | Residue |
| A | GLY151 |
| site_id | AC6 |
| Number of Residues | 2 |
| Details | BINDING SITE FOR RESIDUE IOD A 707 |
| Chain | Residue |
| A | GLY3 |
| A | LYS5 |
| site_id | AC7 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD A 709 |
| Chain | Residue |
| A | SER530 |
| site_id | AC8 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD A 711 |
| Chain | Residue |
| A | LYS18 |
| site_id | AC9 |
| Number of Residues | 2 |
| Details | BINDING SITE FOR RESIDUE IOD A 712 |
| Chain | Residue |
| A | LEU445 |
| A | SER458 |
| site_id | BC1 |
| Number of Residues | 20 |
| Details | BINDING SITE FOR RESIDUE S6P A 713 |
| Chain | Residue |
| A | GLY107 |
| A | GLY108 |
| 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 | HOH812 |
| A | HOH825 |
| A | HOH837 |
| A | HOH849 |
| A | HOH850 |
| site_id | BC2 |
| Number of Residues | 16 |
| Details | BINDING SITE FOR RESIDUE 1YY A 714 |
| Chain | Residue |
| A | HIS9 |
| A | VAL10 |
| A | ILE11 |
| A | TYR24 |
| A | VAL28 |
| A | PRO29 |
| A | GLU32 |
| A | GLY181 |
| A | ARG215 |
| A | HIS504 |
| A | TRP517 |
| A | ALA521 |
| A | GLN524 |
| A | ARG525 |
| A | HOH808 |
| A | HOH848 |
| site_id | BC3 |
| Number of Residues | 3 |
| Details | BINDING SITE FOR RESIDUE GOL A 715 |
| Chain | Residue |
| A | PHE7 |
| A | LYS531 |
| A | HOH846 |
| site_id | BC4 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD B 701 |
| Chain | Residue |
| B | PHE472 |
| site_id | BC5 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD B 703 |
| Chain | Residue |
| B | ARG73 |
| site_id | BC6 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD B 704 |
| Chain | Residue |
| B | THR298 |
| site_id | BC7 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD B 706 |
| Chain | Residue |
| B | GLY151 |
| site_id | BC8 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD B 707 |
| Chain | Residue |
| B | SER530 |
| site_id | BC9 |
| Number of Residues | 2 |
| Details | BINDING SITE FOR RESIDUE IOD B 708 |
| Chain | Residue |
| B | GLY3 |
| B | LYS5 |
| site_id | CC1 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD B 709 |
| Chain | Residue |
| B | ASN196 |
| site_id | CC2 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD B 710 |
| Chain | Residue |
| B | SER458 |
| site_id | CC3 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE IOD B 714 |
| Chain | Residue |
| B | LYS531 |
| site_id | CC4 |
| Number of Residues | 21 |
| Details | BINDING SITE FOR RESIDUE S6P B 715 |
| 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 | HOH827 |
| B | HOH844 |
| B | HOH845 |
| B | HOH850 |
| B | HOH864 |
| B | HOH865 |
| site_id | CC5 |
| Number of Residues | 17 |
| Details | BINDING SITE FOR RESIDUE 1YY B 716 |
| Chain | Residue |
| B | HIS9 |
| B | VAL10 |
| B | ILE11 |
| B | TYR24 |
| B | VAL28 |
| B | PRO29 |
| B | GLU32 |
| B | GLY181 |
| B | ARG215 |
| B | HIS504 |
| B | LYS514 |
| B | TRP517 |
| B | ALA521 |
| B | GLN524 |
| B | ARG525 |
| B | HOH806 |
| B | HOH872 |
| site_id | CC6 |
| Number of Residues | 5 |
| Details | BINDING SITE FOR RESIDUE GOL B 717 |
| Chain | Residue |
| B | SER118 |
| B | VAL119 |
| B | ASN122 |
| B | THR135 |
| B | TYR136 |
| site_id | CC7 |
| Number of Residues | 2 |
| Details | BINDING SITE FOR RESIDUE SO4 B 718 |
| Chain | Residue |
| B | SER321 |
| B | GLU325 |
| site_id | CC8 |
| Number of Residues | 1 |
| Details | BINDING SITE FOR RESIDUE SO4 B 719 |
| Chain | Residue |
| B | ALA44 |
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 |
| A | THR109 | |
| A | SER179 | |
| A | LYS514 | |
| B | THR109 | |
| B | SER179 | |
| B | LYS514 |
| site_id | SWS_FT_FI2 |
| Number of Residues | 4 |
| Details | BINDING: BINDING => ECO:0000269|PubMed:23621087, ECO:0007744|PDB:4BB9 |
| Chain | Residue | Details |
| A | GLU153 | |
| A | GLU348 | |
| B | GLU153 | |
| B | GLU348 |
