Entry | Database: PDB / ID: 6e0e |
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Title | Crystal structure of Glucokinase in complex with compound 6 |
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Components | Glucokinase |
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Keywords | Transferase/Transferase Inhibitor / Glucokinase / glucokinase activator / structure-aided design / structure-based design / type II diabetes / Transferase-Transferase Inhibitor complex |
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Function / homology | Function and homology information
Defective GCK causes maturity-onset diabetes of the young 2 (MODY2) / glucose sensor activity / regulation of potassium ion transport / mannokinase activity / hexokinase / fructokinase activity / carbohydrate phosphorylation / glucose catabolic process / glucokinase activity / glucose 6-phosphate metabolic process ...Defective GCK causes maturity-onset diabetes of the young 2 (MODY2) / glucose sensor activity / regulation of potassium ion transport / mannokinase activity / hexokinase / fructokinase activity / carbohydrate phosphorylation / glucose catabolic process / glucokinase activity / glucose 6-phosphate metabolic process / Regulation of Glucokinase by Glucokinase Regulatory Protein / Defective TPR may confer susceptibility towards thyroid papillary carcinoma (TPC) / NADP metabolic process / D-glucose binding / cellular response to leptin stimulus / calcium ion import / canonical glycolysis / Glycolysis / regulation of glycolytic process / intracellular glucose homeostasis / Regulation of gene expression in beta cells / regulation of insulin secretion / positive regulation of glycogen biosynthetic process / negative regulation of gluconeogenesis / FOXO-mediated transcription of oxidative stress, metabolic and neuronal genes / response to glucose / glycolytic process / positive regulation of insulin secretion / cellular response to insulin stimulus / glucose metabolic process / glucose homeostasis / mitochondrion / nucleoplasm / ATP binding / cytosolSimilarity search - Function Hexokinase; domain 1 / Hexokinase; domain 1 - #20 / Hexokinase / Hexokinase, binding site / Hexokinase, N-terminal / Hexokinase, C-terminal / Hexokinase / Hexokinase / Hexokinase domain signature. / Hexokinase domain profile. ...Hexokinase; domain 1 / Hexokinase; domain 1 - #20 / Hexokinase / Hexokinase, binding site / Hexokinase, N-terminal / Hexokinase, C-terminal / Hexokinase / Hexokinase / Hexokinase domain signature. / Hexokinase domain profile. / ATPase, nucleotide binding domain / ATPase, nucleotide binding domain / Nucleotidyltransferase; domain 5 / 2-Layer Sandwich / 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 / FOURIER SYNTHESIS / Resolution: 2.7 Å |
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Authors | Hinklin, R.J. / Baer, B.R. / Boyd, S.A. / Chicarelli, M.D. / Condroski, K.R. / DeWolf, W.E. / Fischer, J. / Frank, M. / Hingorani, G.P. / Lee, P.A. ...Hinklin, R.J. / Baer, B.R. / Boyd, S.A. / Chicarelli, M.D. / Condroski, K.R. / DeWolf, W.E. / Fischer, J. / Frank, M. / Hingorani, G.P. / Lee, P.A. / Neitzel, N.A. / Pratt, S.A. / Singh, A. / Sullivan, F.X. / Turner, T. / Voegtli, W.C. / Wallace, E.M. / Williams, L. / Aicher, T.D. |
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Citation | Journal: Bioorg.Med.Chem. / Year: 2020 Title: Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Authors: Hinklin, R.J. / Baer, B.R. / Boyd, S.A. / Chicarelli, M.D. / Condroski, K.R. / DeWolf Jr., W.E. / Fischer, J. / Frank, M. / Hingorani, G.P. / Lee, P.A. / Neitzel, N.A. / Pratt, S.A. / Singh, ...Authors: Hinklin, R.J. / Baer, B.R. / Boyd, S.A. / Chicarelli, M.D. / Condroski, K.R. / DeWolf Jr., W.E. / Fischer, J. / Frank, M. / Hingorani, G.P. / Lee, P.A. / Neitzel, N.A. / Pratt, S.A. / Singh, A. / Sullivan, F.X. / Turner, T. / Voegtli, W.C. / Wallace, E.M. / Williams, L. / Aicher, T.D. |
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History | Deposition | Jul 6, 2018 | Deposition site: RCSB / Processing site: RCSB |
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Revision 1.0 | Jul 10, 2019 | Provider: repository / Type: Initial release |
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Revision 1.1 | Jan 22, 2020 | Group: Data collection / Database references / Category: chem_comp / citation / citation_author Item: _chem_comp.type / _citation.country ..._chem_comp.type / _citation.country / _citation.journal_abbrev / _citation.journal_id_ASTM / _citation.journal_id_CSD / _citation.journal_id_ISSN / _citation.journal_volume / _citation.page_first / _citation.page_last / _citation.pdbx_database_id_DOI / _citation.pdbx_database_id_PubMed / _citation.title / _citation.year |
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Revision 1.2 | Jul 29, 2020 | Group: Data collection / Derived calculations / Structure summary Category: chem_comp / entity ...chem_comp / entity / pdbx_chem_comp_identifier / pdbx_entity_nonpoly / struct_site / struct_site_gen Item: _chem_comp.name / _chem_comp.type ..._chem_comp.name / _chem_comp.type / _entity.pdbx_description / _pdbx_entity_nonpoly.name Description: Carbohydrate remediation / Provider: repository / Type: Remediation |
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Revision 1.3 | Mar 13, 2024 | Group: Data collection / Database references / Structure summary Category: chem_comp / chem_comp_atom ...chem_comp / chem_comp_atom / chem_comp_bond / database_2 Item: _chem_comp.pdbx_synonyms / _database_2.pdbx_DOI / _database_2.pdbx_database_accession |
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