Entry | Database: PDB / ID: 5clm |
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Title | 1,4-Oxazine BACE1 inhibitors |
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Components | Beta-secretase 1 |
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Keywords | HYDROLASE / BACE1 PROTEASE Inhibitor / orally bioavailable / brain penetrant / PROTEROS BIOSTRUCTURES GMBH |
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Function / homology | Function and homology information
memapsin 2 / Golgi-associated vesicle lumen / signaling receptor ligand precursor processing / beta-aspartyl-peptidase activity / amyloid precursor protein catabolic process / amyloid-beta formation / membrane protein ectodomain proteolysis / cellular response to manganese ion / amyloid-beta metabolic process / prepulse inhibition ...memapsin 2 / Golgi-associated vesicle lumen / signaling receptor ligand precursor processing / beta-aspartyl-peptidase activity / amyloid precursor protein catabolic process / amyloid-beta formation / membrane protein ectodomain proteolysis / cellular response to manganese ion / amyloid-beta metabolic process / prepulse inhibition / detection of mechanical stimulus involved in sensory perception of pain / protein serine/threonine kinase binding / cellular response to copper ion / presynaptic modulation of chemical synaptic transmission / hippocampal mossy fiber to CA3 synapse / multivesicular body / response to lead ion / trans-Golgi network / recycling endosome / protein processing / cellular response to amyloid-beta / positive regulation of neuron apoptotic process / synaptic vesicle / late endosome / peptidase activity / amyloid-beta binding / endopeptidase activity / amyloid fibril formation / aspartic-type endopeptidase activity / lysosome / early endosome / endosome membrane / endosome / membrane raft / Amyloid fiber formation / endoplasmic reticulum lumen / axon / neuronal cell body / dendrite / Golgi apparatus / enzyme binding / cell surface / proteolysis / membrane / plasma membraneSimilarity search - Function Beta-secretase BACE1 / Beta-secretase BACE / Memapsin-like / Eukaryotic aspartyl protease / Aspartic peptidase A1 family / Peptidase family A1 domain / Peptidase family A1 domain profile. / Cathepsin D, subunit A; domain 1 / Acid Proteases / Aspartic peptidase, active site ...Beta-secretase BACE1 / Beta-secretase BACE / Memapsin-like / Eukaryotic aspartyl protease / Aspartic peptidase A1 family / Peptidase family A1 domain / Peptidase family A1 domain profile. / Cathepsin D, subunit A; domain 1 / Acid Proteases / Aspartic peptidase, active site / Eukaryotic and viral aspartyl proteases active site. / Aspartic peptidase domain superfamily / Beta Barrel / Mainly BetaSimilarity search - Domain/homology |
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Biological species | Homo sapiens (human) |
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Method | X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution: 2.61 Å |
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Authors | Rombouts, F. / Tresadern, G. / Delgado, O. / Martinez Lamenca, C. / Van Gool, M. / Garcia-Molina, A. / Alonso De Diego, S. / Oehlrich, D. / Prokopcova, H. / Alonso, J.M. ...Rombouts, F. / Tresadern, G. / Delgado, O. / Martinez Lamenca, C. / Van Gool, M. / Garcia-Molina, A. / Alonso De Diego, S. / Oehlrich, D. / Prokopcova, H. / Alonso, J.M. / Austin, N. / Borghys, H. / Van Brandt, S. / Surkyn, M. / De Cleyn, M. / Vos, A. / Alexander, R. / MacDonald, G. / Moechars, D. / Trabanco, A. / Gijsen, H. |
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Citation | Journal: J.Med.Chem. / Year: 2015 Title: 1,4-Oxazine beta-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads. Authors: Rombouts, F.J. / Tresadern, G. / Delgado, O. / Martinez-Lamenca, C. / Van Gool, M. / Garcia-Molina, A. / Alonso de Diego, S.A. / Oehlrich, D. / Prokopcova, H. / Alonso, J.M. / Austin, N. / ...Authors: Rombouts, F.J. / Tresadern, G. / Delgado, O. / Martinez-Lamenca, C. / Van Gool, M. / Garcia-Molina, A. / Alonso de Diego, S.A. / Oehlrich, D. / Prokopcova, H. / Alonso, J.M. / Austin, N. / Borghys, H. / Van Brandt, S. / Surkyn, M. / De Cleyn, M. / Vos, A. / Alexander, R. / Macdonald, G. / Moechars, D. / Gijsen, H. / Trabanco, A.A. |
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History | Deposition | Jul 16, 2015 | Deposition site: RCSB / Processing site: PDBE |
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Revision 1.0 | Sep 30, 2015 | Provider: repository / Type: Initial release |
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Revision 1.1 | Nov 4, 2015 | Group: Database references |
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