- PDB-4pxs: Human GKRP bound to AMG-0265 (N-[(R)-(2-CHLOROPHENYL){7-[4-(2-HYD... -
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ID or keywords:
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Basic information
Entry
Database: PDB / ID: 4pxs
Title
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
Components
Glucokinase regulatory protein
Keywords
transferase/transferase inhibitor / SIS domain containing protein / GKRP binds to and inhibits Glucokinase activity / Glucokinase / Liver / transferase-transferase inhibitor complex
Function / homology
Function and homology information
amino sugar catabolic process / ether hydrolase activity / carbon-oxygen lyase activity / negative regulation of glucokinase activity / glucose sensor activity / fructose-6-phosphate binding / urate metabolic process / kinase inhibitor activity / peptidoglycan turnover / Regulation of Glucokinase by Glucokinase Regulatory Protein ...amino sugar catabolic process / ether hydrolase activity / carbon-oxygen lyase activity / negative regulation of glucokinase activity / glucose sensor activity / fructose-6-phosphate binding / urate metabolic process / kinase inhibitor activity / peptidoglycan turnover / Regulation of Glucokinase by Glucokinase Regulatory Protein / Defective TPR may confer susceptibility towards thyroid papillary carcinoma (TPC) / response to fructose / triglyceride homeostasis / enzyme inhibitor activity / response to glucose / protein import into nucleus / glucose homeostasis / carbohydrate binding / enzyme binding / mitochondrion / nucleoplasm / cytoplasm / cytosol Similarity search - Function
C-terminal lid domain of glucokinase regulatory protein / Glucokinase regulatory protein, conserved site / N-acetylmuramic acid 6-phosphate etherase/glucokinase regulatory protein / Glucokinase regulatory protein family signature. / SIS domain / SIS domain profile. / SIS domain superfamily / Glucose-6-phosphate isomerase like protein; domain 1 / Rossmann fold / 3-Layer(aba) Sandwich / Alpha Beta Similarity search - Domain/homology
Resolution: 2.6→37 Å / Cor.coef. Fo:Fc: 0.937 / Cor.coef. Fo:Fc free: 0.905 / SU B: 14.338 / SU ML: 0.297 / Cross valid method: THROUGHOUT / ESU R: 0.609 / ESU R Free: 0.366 / Stereochemistry target values: MAXIMUM LIKELIHOOD / Details: HYDROGENS HAVE BEEN ADDED IN THE RIDING POSITIONS
Rfactor
Num. reflection
% reflection
Selection details
Rfree
0.3072
2527
5.1 %
RANDOM
Rwork
0.23423
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obs
0.23798
47141
96.68 %
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Solvent computation
Ion probe radii: 0.8 Å / Shrinkage radii: 0.8 Å / VDW probe radii: 1.2 Å / Solvent model: MASK