Entry | Database: PDB / ID: 4mro |
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Title | Human GKRP bound to AMG-5980 and S6P |
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Components | Glucokinase regulatory protein |
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Keywords | Transferase Inhibitor / SIS domains / Regulatory protein / Glucokinase / phospho-fructose |
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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 / cytosolSimilarity 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 BetaSimilarity search - Domain/homology |
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Biological species | Homo sapiens (human) |
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Method | X-RAY DIFFRACTION / MOLECULAR REPLACEMENT / Resolution: 2.2 Å |
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Authors | St Jean, D.J. / Ashton, K.S. / Bartberger, M.D. / Chen, J. / Chmait, S. / Cupples, R. / Galbreath, E. / Helmering, J. / Jordan, S.R. / Liu, L. ...St Jean, D.J. / Ashton, K.S. / Bartberger, M.D. / Chen, J. / Chmait, S. / Cupples, R. / Galbreath, E. / Helmering, J. / Jordan, S.R. / Liu, L. / Kunz, K. / Michelsen, K. / Nishimura, N. / Pennington, L.D. / Poon, S.F. / Sivits, G. / Stec, M.M. / Tamayo, N. / Van, G. / Yang, K. / Norman, M.H. / Fotsch, C. / LLoyd, D.J. / Hale, C. |
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Citation | Journal: J.Med.Chem. / Year: 2014 Title: Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. Authors: St Jean, D.J. / Ashton, K.S. / Bartberger, M.D. / Chen, J. / Chmait, S. / Cupples, R. / Galbreath, E. / Helmering, J. / Hong, F.T. / Jordan, S.R. / Liu, L. / Kunz, R.K. / Michelsen, K. / ...Authors: St Jean, D.J. / Ashton, K.S. / Bartberger, M.D. / Chen, J. / Chmait, S. / Cupples, R. / Galbreath, E. / Helmering, J. / Hong, F.T. / Jordan, S.R. / Liu, L. / Kunz, R.K. / Michelsen, K. / Nishimura, N. / Pennington, L.D. / Poon, S.F. / Reid, D. / Sivits, G. / Stec, M.M. / Tadesse, S. / Tamayo, N. / Van, G. / Yang, K.C. / Zhang, J. / Norman, M.H. / Fotsch, C. / Lloyd, D.J. / Hale, C. |
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History | Deposition | Sep 17, 2013 | Deposition site: RCSB / Processing site: RCSB |
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Revision 1.0 | May 7, 2014 | Provider: repository / Type: Initial release |
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Revision 1.1 | Feb 28, 2024 | Group: Data collection / Database references ...Data collection / Database references / Derived calculations / Structure summary Category: chem_comp / chem_comp_atom ...chem_comp / chem_comp_atom / chem_comp_bond / database_2 / struct_ref_seq_dif / struct_site Item: _chem_comp.pdbx_synonyms / _database_2.pdbx_DOI ..._chem_comp.pdbx_synonyms / _database_2.pdbx_DOI / _database_2.pdbx_database_accession / _struct_ref_seq_dif.details / _struct_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id |
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Revision 1.2 | Apr 3, 2024 | Group: Refinement description / Category: pdbx_initial_refinement_model |
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