Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 최선 | * |
dc.date.accessioned | 2018-04-25T08:13:28Z | - |
dc.date.available | 2018-04-25T08:13:28Z | - |
dc.date.issued | 2018 | * |
dc.identifier.issn | 0968-0896 | * |
dc.identifier.issn | 1464-3391 | * |
dc.identifier.other | OAK-22099 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/242507 | - |
dc.description.abstract | Pyroglutamate-modified amyloid beta peptides (pGlu-A beta) are highly neurotoxic and promote the formation of amyloid plaques. The pGlu-A beta peptides are generated by glutaminyl cyclase (QC), and recent clinical studies indicate that QC represents an alternative therapeutic target to treat Alzheimer's disease (AD). We have previously developed a series of QC inhibitors with an extended pharmacophoric scaffold, termed the Arg-mimetic D-region. In the present study, we focused on the structure activity relationship (SAR) of analogues with modifications in the D-region and evaluated their biological activity. Most compounds in this series exhibited potent activity in vitro, and our SAR analysis and the molecular docking studies identified compound 202 as a potential candidate because it forms an additional hydrophobic interaction in the hQC active site. Overall, our study provides valuable insights into the Arg-mimetic pharmacophore that will guide the design of novel QC inhibitors as potential treatments for AD. (C) 2018 Elsevier Ltd. All rights reserved. | * |
dc.language | English | * |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | * |
dc.subject | Glutaminyl cyclase inhibitor | * |
dc.subject | Alzheimer's disease | * |
dc.subject | Beta-amyloid | * |
dc.title | Potent human glutaminyl cyclase inhibitors as potential anti-Alzheimer's agents: Structure-activity relationship study of Arg-mimetic region | * |
dc.type | Article | * |
dc.relation.issue | 5 | * |
dc.relation.volume | 26 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 1035 | * |
dc.relation.lastpage | 1049 | * |
dc.relation.journaltitle | BIOORGANIC & MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1016/j.bmc.2018.01.015 | * |
dc.identifier.wosid | WOS:000425552300006 | * |
dc.identifier.scopusid | 2-s2.0-85041585109 | * |
dc.author.google | Ngo, Van T. H. | * |
dc.author.google | Van-Hai Hoang | * |
dc.author.google | Phuong-Thao Tran | * |
dc.author.google | Ann, Jihyae | * |
dc.author.google | Cui, Minghua | * |
dc.author.google | Park, Gyungseo | * |
dc.author.google | Choi, Sun | * |
dc.author.google | Lee, Jiyoun | * |
dc.author.google | Kim, Hee | * |
dc.author.google | Ha, Hee-Jin | * |
dc.author.google | Choi, Kwanghyun | * |
dc.author.google | Kim, Young-Ho | * |
dc.author.google | Lee, Jeewoo | * |
dc.contributor.scopusid | 최선(8659831000) | * |
dc.date.modifydate | 20240305081003 | * |