Entry | Database: PDB / ID: 5tl9 |
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Title | crystal structure of mPGES-1 bound to inhibitor |
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Components | Prostaglandin E synthase |
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Keywords | Membrane Protein / Transferase / prostaglandin / enzyme / integral membrane protein / alpha helix / mPGES1 - ligand 0 |
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Function / homology | Function and homology information
regulation of fever generation / prostaglandin-E synthase / prostaglandin-E synthase activity / prostaglandin-D synthase activity / positive regulation of prostaglandin secretion / glutathione binding / Synthesis of Prostaglandins (PG) and Thromboxanes (TX) / glutathione peroxidase activity / prostaglandin biosynthetic process / prostaglandin metabolic process ...regulation of fever generation / prostaglandin-E synthase / prostaglandin-E synthase activity / prostaglandin-D synthase activity / positive regulation of prostaglandin secretion / glutathione binding / Synthesis of Prostaglandins (PG) and Thromboxanes (TX) / glutathione peroxidase activity / prostaglandin biosynthetic process / prostaglandin metabolic process / nuclear envelope lumen / glutathione transferase / glutathione transferase activity / Oxidoreductases; Acting on a peroxide as acceptor; Peroxidases / sensory perception of pain / regulation of inflammatory response / cell population proliferation / negative regulation of cell population proliferation / endoplasmic reticulum membrane / perinuclear region of cytoplasm / signal transduction / membraneSimilarity search - Function Microsomal glutathione S-transferase 1-like / Membrane associated eicosanoid/glutathione metabolism-like domain / Membrane-associated, eicosanoid/glutathione metabolism (MAPEG) protein / Membrane associated eicosanoid/glutathione metabolism-like domain superfamily / MAPEG family / Four Helix Bundle (Hemerythrin (Met), subunit A) / Up-down Bundle / Mainly AlphaSimilarity search - Domain/homology |
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Biological species | Homo sapiens (human) |
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Method | X-RAY DIFFRACTION / SYNCHROTRON / Resolution: 1.2 Å |
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Authors | Luz, J.G. / Antonysamy, S. / Partridge, K. / Fisher, M. |
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Funding support | United States, 1items Organization | Grant number | Country |
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Department of Energy (DOE, United States) | DE-AC02-06CH11357 | United States |
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Citation | Journal: Bioorg. Med. Chem. Lett. / Year: 2017 Title: Discovery and characterization of [(cyclopentyl)ethyl]benzoic acid inhibitors of microsomal prostaglandin E synthase-1. Authors: Partridge, K.M. / Antonysamy, S. / Bhattachar, S.N. / Chandrasekhar, S. / Fisher, M.J. / Fretland, A. / Gooding, K. / Harvey, A. / Hughes, N.E. / Kuklish, S.L. / Luz, J.G. / Manninen, P.R. / ...Authors: Partridge, K.M. / Antonysamy, S. / Bhattachar, S.N. / Chandrasekhar, S. / Fisher, M.J. / Fretland, A. / Gooding, K. / Harvey, A. / Hughes, N.E. / Kuklish, S.L. / Luz, J.G. / Manninen, P.R. / McGee, J.E. / Mudra, D.R. / Navarro, A. / Norman, B.H. / Quimby, S.J. / Schiffler, M.A. / Sloan, A.V. / Warshawsky, A.M. / Weller, J.M. / York, J.S. / Yu, X.P. |
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History | Deposition | Oct 10, 2016 | Deposition site: RCSB / Processing site: RCSB |
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Revision 1.0 | Mar 1, 2017 | Provider: repository / Type: Initial release |
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Revision 1.1 | Mar 15, 2017 | Group: Database references |
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Revision 1.2 | Sep 6, 2017 | Group: Author supporting evidence / Category: pdbx_audit_support / Item: _pdbx_audit_support.funding_organization |
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Revision 1.3 | Dec 4, 2019 | Group: Author supporting evidence / Category: pdbx_audit_support / Item: _pdbx_audit_support.funding_organization |
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Revision 1.4 | 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.mon_nstd_flag / _chem_comp.name ..._chem_comp.mon_nstd_flag / _chem_comp.name / _chem_comp.type / _entity.pdbx_description / _pdbx_entity_nonpoly.name Description: Carbohydrate remediation / Provider: repository / Type: Remediation |
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