PubMed:28825789
Annnotations
PubMed_ArguminSci
| Id | Subject | Object | Predicate | Lexical cue |
|---|---|---|---|---|
| T1 | 141-330 | DRI_Background | denotes | e report the synthesis and pharmacological investigation of analogs of the endogenous molecule kynurenic acid (KYNA) as multifunctional agents for the treatment of Alzheimer's disease (AD). |
| T2 | 331-710 | DRI_Outcome | denotes | Synthesized KYNA analogs were tested for their N-methyl-D-aspartate (NMDA) receptor binding, mGluR5 binding and function, acetylcholinesterase (AChE) inhibition, DPPH radical scavenging, interference with the amyloid beta peptide (Aβ) fibrillation process, and protection against Aβ-induced toxicity in transgenic Caenorhabditis elegans strain GMC101 expressing full-length Aβ42. |
| T3 | 711-840 | DRI_Background | denotes | Molecular modeling studies were also performed to predict the binding modes of most active compounds with NMDAR, mGluR5 and Aβ42. |
| T4 | 841-1068 | DRI_Outcome | denotes | Among the synthesized analogs, 3c, 5b and 5c emerged as multifunctional compounds that act via multiple anti-AD mechanisms including AChE inhibition, free radical scavenging, NMDA receptor binding, mGluR5 binding, inhibition of |
| T5 | 1081-1134 | DRI_Outcome | denotes | formation, and disassembly of preformed Aβ42 fibrils. |
| T6 | 1135-1240 | DRI_Outcome | denotes | Interestingly, 5c showed protection against Aβ42-induced toxicity in transgenic C. elegans strain GMC101. |
| T7 | 1241-1357 | DRI_Background | denotes | Moreover, 5b and 5c displayed high permeability in an MDR1-MDCKII cell-based model of the blood-brain barrier (BBB). |
| T8 | 1358-1483 | DRI_Background | denotes | Compound 3b emerged with specific activity as a mi-cromolar AChE inhibitor, however it had low permeability in the BBB model. |
| T9 | 1484-1627 | DRI_Outcome | denotes | This study highlights the opportunities that exist to develop analogs of endogenous molecules from the kynurenine pathway for therapeutic uses. |
Goldhamster2_Cellosaurus
| Id | Subject | Object | Predicate | Lexical cue |
|---|---|---|---|---|
| T1 | 140-142 | CVCL_5M23|Cancer_cell_line|Mesocricetus auratus | denotes | We |
| T2 | 326-328 | CVCL_M606|Cancer_cell_line|Homo sapiens | denotes | AD |
| T3 | 548-552 | CVCL_R799|Transformed_cell_line|Gorilla gorilla gorilla | denotes | beta |
| T4 | 562-563 | CVCL_6479|Finite_cell_line|Mus musculus | denotes | A |
| T5 | 611-612 | CVCL_6479|Finite_cell_line|Mus musculus | denotes | A |
| T6 | 705-706 | CVCL_6479|Finite_cell_line|Mus musculus | denotes | A |
| T7 | 795-801 | CVCL_C410|Hybridoma|Mus musculus | denotes | active |
| T8 | 835-836 | CVCL_6479|Finite_cell_line|Mus musculus | denotes | A |
| T9 | 883-885 | CVCL_DC70|Cancer_cell_line|Homo sapiens | denotes | 5c |
| T10 | 950-952 | CVCL_M606|Cancer_cell_line|Homo sapiens | denotes | AD |
| T11 | 1069-1070 | CVCL_6479|Finite_cell_line|Mus musculus | denotes | A |
| T12 | 1121-1122 | CVCL_6479|Finite_cell_line|Mus musculus | denotes | A |
| T13 | 1150-1152 | CVCL_DC70|Cancer_cell_line|Homo sapiens | denotes | 5c |
| T14 | 1179-1180 | CVCL_6479|Finite_cell_line|Mus musculus | denotes | A |
| T15 | 1215-1216 | CVCL_S361|Finite_cell_line|Mus musculus | denotes | C |
| T16 | 1258-1260 | CVCL_DC70|Cancer_cell_line|Homo sapiens | denotes | 5c |
| T17 | 1292-1294 | CVCL_8754|Cancer_cell_line|Homo sapiens | denotes | an |
| T18 | 1292-1294 | CVCL_H241|Cancer_cell_line|Homo sapiens | denotes | an |
| T19 | 1300-1306 | CVCL_0424|Spontaneously_immortalized_cell_line|Canis lupus familiaris | denotes | MDCKII |
| T20 | 1392-1400 | CVCL_C410|Hybridoma|Mus musculus | denotes | activity |
| T21 | 1404-1405 | CVCL_6479|Finite_cell_line|Mus musculus | denotes | a |
| T22 | 1406-1408 | CVCL_0C76|Cancer_cell_line|Canis lupus familiaris | denotes | mi |
GoldHamster
| Id | Subject | Object | Predicate | Lexical cue |
|---|---|---|---|---|
| T1 | 27-41 | CHEBI:18344 | denotes | kynurenic acid |
| T2 | 27-41 | D007736 | denotes | kynurenic acid |
| T3 | 27-41 | D007736 | denotes | kynurenic acid |
| T9 | 63-82 | D000544 | denotes | Alzheimer's disease |
| T10 | 63-82 | D000544 | denotes | Alzheimer's disease |
| T13 | 154-163 | GO:0009058 | denotes | synthesis |
| T14 | 227-235 | CHEBI:25367 | denotes | molecule |
| T15 | 236-250 | CHEBI:18344 | denotes | kynurenic acid |
| T16 | 236-250 | D007736 | denotes | kynurenic acid |
| T17 | 236-250 | D007736 | denotes | kynurenic acid |
| T23 | 305-324 | D000544 | denotes | Alzheimer's disease |
| T24 | 305-324 | D000544 | denotes | Alzheimer's disease |
| T27 | 378-398 | D016202 | denotes | N-methyl-D-aspartate |
| T28 | 378-398 | D016202 | denotes | N-methyl-D-aspartate |
| T29 | 378-398 | CHEBI:31882 | denotes | N-methyl-D-aspartate |
| T39 | 389-398 | 42543 | denotes | aspartate |
| T42 | 400-404 | D016202 | denotes | NMDA |
| T43 | 400-404 | CHEBI:6121 | denotes | NMDA |
| T44 | 400-404 | D016202 | denotes | NMDA |
| T45 | 400-404 | CHEBI:31882 | denotes | NMDA |
| T46 | 400-414 | GO:0004972 | denotes | NMDA) receptor |
| T47 | 406-422 | GO:0005102 | denotes | receptor binding |
| T48 | 415-422 | SO:0100018 | denotes | binding |
| T49 | 415-422 | SO:0001091 | denotes | binding |
| T52 | 424-430 | Q3UVX5 | denotes | mGluR5 |
| T53 | 424-430 | PR:P41594 | denotes | mGluR5 |
| T54 | 424-430 | P31424 | denotes | mGluR5 |
| T55 | 424-430 | PR:P31424 | denotes | mGluR5 |
| T56 | 424-430 | PR:000008267 | denotes | mGluR5 |
| T57 | 424-430 | P41594 | denotes | mGluR5 |
| T58 | 424-430 | PR:Q3UVX5 | denotes | mGluR5 |
| T59 | 431-438 | SO:0100018 | denotes | binding |
| T60 | 431-438 | SO:0001091 | denotes | binding |
| T61 | 431-438 | GO:0005488 | denotes | binding |
| T62 | 453-473 | P21836 | denotes | acetylcholinesterase |
| T63 | 453-473 | Q27677 | denotes | acetylcholinesterase |
| T65 | 453-473 | P37136 | denotes | acetylcholinesterase |
| T66 | 453-473 | Q7LZG1 | denotes | acetylcholinesterase |
| T67 | 453-473 | P07692 | denotes | acetylcholinesterase |
| T68 | 453-473 | Q9DDE3 | denotes | acetylcholinesterase |
| T69 | 453-473 | Q92081 | denotes | acetylcholinesterase |
| T70 | 453-473 | P07140 | denotes | acetylcholinesterase |
| T71 | 453-473 | Q86GC9 | denotes | acetylcholinesterase |
| T72 | 453-473 | Q869C3 | denotes | acetylcholinesterase |
| T73 | 453-473 | P22303 | denotes | acetylcholinesterase |
| T74 | 453-473 | P23795 | denotes | acetylcholinesterase |
| T75 | 453-473 | P56161 | denotes | acetylcholinesterase |
| T76 | 453-473 | P36196 | denotes | acetylcholinesterase |
| T77 | 453-473 | Q92035 | denotes | acetylcholinesterase |
| T78 | 453-473 | O42275 | denotes | acetylcholinesterase |
| T79 | 453-473 | P04058 | denotes | acetylcholinesterase |
| T80 | 453-473 | Q29499 | denotes | acetylcholinesterase |
| T81 | 453-473 | Q867X2 | denotes | acetylcholinesterase |
| T82 | 453-473 | O62763 | denotes | acetylcholinesterase |
| T83 | 453-473 | Q867X3 | denotes | acetylcholinesterase |
| T84 | 453-473 | PR:000003626 | denotes | acetylcholinesterase |
| T85 | 453-473 | Q86GC8 | denotes | acetylcholinesterase |
| T64 | 453-473 | D000110 | denotes | acetylcholinesterase |
| T86 | 475-479 | P21836 | denotes | AChE |
| T87 | 475-479 | PR:P37136 | denotes | AChE |
| T89 | 475-479 | Q27677 | denotes | AChE |
| T90 | 475-479 | P37136 | denotes | AChE |
| T91 | 475-479 | Q7LZG1 | denotes | AChE |
| T92 | 475-479 | P07692 | denotes | AChE |
| T93 | 475-479 | PR:Q9DDE3 | denotes | AChE |
| T94 | 475-479 | Q9DDE3 | denotes | AChE |
| T95 | 475-479 | PR:P21836 | denotes | AChE |
| T96 | 475-479 | Q92081 | denotes | AChE |
| T97 | 475-479 | P07140 | denotes | AChE |
| T98 | 475-479 | Q86GC9 | denotes | AChE |
| T100 | 475-479 | Q869C3 | denotes | AChE |
| T101 | 475-479 | P22303 | denotes | AChE |
| T102 | 475-479 | P23795 | denotes | AChE |
| T103 | 475-479 | W4VSJ0 | denotes | AChE |
| T104 | 475-479 | P56161 | denotes | AChE |
| T105 | 475-479 | P36196 | denotes | AChE |
| T106 | 475-479 | O42275 | denotes | AChE |
| T107 | 475-479 | P04058 | denotes | AChE |
| T108 | 475-479 | Q29499 | denotes | AChE |
| T109 | 475-479 | Q867X2 | denotes | AChE |
| T110 | 475-479 | PR:P36196 | denotes | AChE |
| T111 | 475-479 | O62763 | denotes | AChE |
| T112 | 475-479 | Q867X3 | denotes | AChE |
| T113 | 475-479 | PR:000003626 | denotes | AChE |
| T114 | 475-479 | Q86GC8 | denotes | AChE |
| T115 | 475-479 | PR:P22303 | denotes | AChE |
| T88 | 475-479 | D010146 | denotes | AChE |
| T99 | 475-479 | D010146 | denotes | AChE |
| T116 | 498-505 | CHEBI:26519 | denotes | radical |
| T120 | 540-560 | PR:000036193 | denotes | amyloid beta peptide |
| T119 | 540-560 | D016229 | denotes | amyloid beta peptide |
| T121 | 540-560 | D016229 | denotes | amyloid beta peptide |
| T124 | 553-560 | SO:0001064 | denotes | peptide |
| T128 | 553-563 | C098708 | denotes | peptide (A |
| T129 | 634-644 | SO:0000781 | denotes | transgenic |
| T131 | 645-667 | D017173 | denotes | Caenorhabditis elegans |
| T132 | 645-667 | 6239 | denotes | Caenorhabditis elegans |
| T133 | 773-780 | SO:0100018 | denotes | binding |
| T134 | 773-780 | SO:0001091 | denotes | binding |
| T135 | 773-780 | GO:0005488 | denotes | binding |
| T137 | 824-830 | Q3UVX5 | denotes | mGluR5 |
| T138 | 824-830 | PR:P41594 | denotes | mGluR5 |
| T139 | 824-830 | P31424 | denotes | mGluR5 |
| T140 | 824-830 | PR:P31424 | denotes | mGluR5 |
| T141 | 824-830 | PR:000008267 | denotes | mGluR5 |
| T142 | 824-830 | P41594 | denotes | mGluR5 |
| T143 | 824-830 | PR:Q3UVX5 | denotes | mGluR5 |
| T144 | 872-877 | CVCL_5L00 | denotes | 3c, 5 |
| T145 | 872-877 | CVCL_KB11 | denotes | 3c, 5 |
| T146 | 974-978 | P21836 | denotes | AChE |
| T147 | 974-978 | PR:P37136 | denotes | AChE |
| T149 | 974-978 | Q27677 | denotes | AChE |
| T150 | 974-978 | P37136 | denotes | AChE |
| T151 | 974-978 | Q7LZG1 | denotes | AChE |
| T152 | 974-978 | P07692 | denotes | AChE |
| T153 | 974-978 | PR:Q9DDE3 | denotes | AChE |
| T154 | 974-978 | Q9DDE3 | denotes | AChE |
| T155 | 974-978 | PR:P21836 | denotes | AChE |
| T156 | 974-978 | Q92081 | denotes | AChE |
| T157 | 974-978 | P07140 | denotes | AChE |
| T158 | 974-978 | Q86GC9 | denotes | AChE |
| T160 | 974-978 | Q869C3 | denotes | AChE |
| T161 | 974-978 | P22303 | denotes | AChE |
| T162 | 974-978 | P23795 | denotes | AChE |
| T163 | 974-978 | W4VSJ0 | denotes | AChE |
| T164 | 974-978 | P56161 | denotes | AChE |
| T165 | 974-978 | P36196 | denotes | AChE |
| T166 | 974-978 | O42275 | denotes | AChE |
| T167 | 974-978 | P04058 | denotes | AChE |
| T168 | 974-978 | Q29499 | denotes | AChE |
| T169 | 974-978 | Q867X2 | denotes | AChE |
| T170 | 974-978 | PR:P36196 | denotes | AChE |
| T171 | 974-978 | O62763 | denotes | AChE |
| T172 | 974-978 | Q867X3 | denotes | AChE |
| T173 | 974-978 | PR:000003626 | denotes | AChE |
| T174 | 974-978 | Q86GC8 | denotes | AChE |
| T175 | 974-978 | PR:P22303 | denotes | AChE |
| T148 | 974-978 | D010146 | denotes | AChE |
| T159 | 974-978 | D010146 | denotes | AChE |
| T176 | 991-1003 | CHEBI:26519 | denotes | free radical |
| T178 | 1016-1020 | D016202 | denotes | NMDA |
| T179 | 1016-1020 | CHEBI:6121 | denotes | NMDA |
| T180 | 1016-1020 | D016202 | denotes | NMDA |
| T181 | 1016-1020 | CHEBI:31882 | denotes | NMDA |
| T182 | 1016-1029 | GO:0004972 | denotes | NMDA receptor |
| T183 | 1021-1037 | GO:0005102 | denotes | receptor binding |
| T184 | 1030-1037 | SO:0100018 | denotes | binding |
| T185 | 1030-1037 | SO:0001091 | denotes | binding |
| T188 | 1039-1045 | Q3UVX5 | denotes | mGluR5 |
| T189 | 1039-1045 | PR:P41594 | denotes | mGluR5 |
| T190 | 1039-1045 | P31424 | denotes | mGluR5 |
| T191 | 1039-1045 | PR:P31424 | denotes | mGluR5 |
| T192 | 1039-1045 | PR:000008267 | denotes | mGluR5 |
| T193 | 1039-1045 | P41594 | denotes | mGluR5 |
| T194 | 1039-1045 | PR:Q3UVX5 | denotes | mGluR5 |
| T195 | 1046-1053 | SO:0100018 | denotes | binding |
| T196 | 1046-1053 | SO:0001091 | denotes | binding |
| T197 | 1046-1053 | GO:0005488 | denotes | binding |
| T198 | 1074-1080 | GO:0099512 | denotes | fibril |
| T199 | 1081-1090 | GO:0009058 | denotes | formation |
| T200 | 1204-1214 | SO:0000781 | denotes | transgenic |
| T201 | 1295-1298 | CHEBI:53218 | denotes | MDR |
| T202 | 1295-1298 | GO:0004745 | denotes | MDR |
| T203 | 1295-1299 | PR:P53258 | denotes | MDR1 |
| T204 | 1295-1299 | PR:P43245 | denotes | MDR1 |
| T205 | 1295-1299 | PR:P08183 | denotes | MDR1 |
| T206 | 1295-1299 | PR:P06795 | denotes | MDR1 |
| T207 | 1295-1299 | PR:Q9ZR72 | denotes | MDR1 |
| T208 | 1295-1299 | PR:000033662 | denotes | MDR1 |
| T209 | 1295-1299 | PR:Q5ABU7 | denotes | MDR1 |
| T210 | 1295-1299 | PR:Q91WV0 | denotes | MDR1 |
| T211 | 1295-1299 | PR:000001891 | denotes | MDR1 |
| T212 | 1295-1299 | PR:Q9LJX0 | denotes | MDR1 |
| T213 | 1300-1306 | CVCL_0424 | denotes | MDCKII |
| T214 | 1331-1350 | UBERON:0000120 | denotes | blood-brain barrier |
| T217 | 1352-1355 | UBERON:0000120 | denotes | BBB |
| T218 | 1418-1422 | P21836 | denotes | AChE |
| T219 | 1418-1422 | PR:P37136 | denotes | AChE |
| T221 | 1418-1422 | Q27677 | denotes | AChE |
| T222 | 1418-1422 | P37136 | denotes | AChE |
| T223 | 1418-1422 | Q7LZG1 | denotes | AChE |
| T224 | 1418-1422 | P07692 | denotes | AChE |
| T225 | 1418-1422 | PR:Q9DDE3 | denotes | AChE |
| T226 | 1418-1422 | Q9DDE3 | denotes | AChE |
| T227 | 1418-1422 | PR:P21836 | denotes | AChE |
| T228 | 1418-1422 | Q92081 | denotes | AChE |
| T229 | 1418-1422 | P07140 | denotes | AChE |
| T230 | 1418-1422 | Q86GC9 | denotes | AChE |
| T232 | 1418-1422 | Q869C3 | denotes | AChE |
| T233 | 1418-1422 | P22303 | denotes | AChE |
| T234 | 1418-1422 | P23795 | denotes | AChE |
| T235 | 1418-1422 | W4VSJ0 | denotes | AChE |
| T236 | 1418-1422 | P56161 | denotes | AChE |
| T237 | 1418-1422 | P36196 | denotes | AChE |
| T238 | 1418-1422 | O42275 | denotes | AChE |
| T239 | 1418-1422 | P04058 | denotes | AChE |
| T240 | 1418-1422 | Q29499 | denotes | AChE |
| T241 | 1418-1422 | Q867X2 | denotes | AChE |
| T242 | 1418-1422 | PR:P36196 | denotes | AChE |
| T243 | 1418-1422 | O62763 | denotes | AChE |
| T244 | 1418-1422 | Q867X3 | denotes | AChE |
| T245 | 1418-1422 | PR:000003626 | denotes | AChE |
| T246 | 1418-1422 | Q86GC8 | denotes | AChE |
| T247 | 1418-1422 | PR:P22303 | denotes | AChE |
| T220 | 1418-1422 | D010146 | denotes | AChE |
| T231 | 1418-1422 | D010146 | denotes | AChE |
| T248 | 1423-1432 | CHEBI:35222 | denotes | inhibitor |
| T249 | 1473-1476 | UBERON:0000120 | denotes | BBB |
| T250 | 1568-1577 | CHEBI:25367 | denotes | molecules |
| T251 | 1587-1597 | CHEBI:16946 | denotes | kynurenine |
| T252 | 1587-1597 | D007737 | denotes | kynurenine |
| T253 | 1587-1597 | CHEBI:28683 | denotes | kynurenine |
| T254 | 1587-1597 | D007737 | denotes | kynurenine |
| T255 | 1598-1605 | CHEBI:34922 | denotes | pathway |
| T256 | 1610-1626 | D045506 | denotes | therapeutic uses |
| T257 | 1610-1626 | D045506 | denotes | therapeutic uses |