Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 김영미 | - |
dc.date.accessioned | 2023-05-17T01:14:26Z | - |
dc.date.available | 2023-05-17T01:14:26Z | - |
dc.date.issued | 2020-12 | - |
dc.identifier.citation | Journal of Medicinal Chemistry, v. 63, NO. 24, Page. 16012.0-16027.0 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c01874 | en_US |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/180572 | - |
dc.description.abstract | Following our report that A3 adenosine receptor (AR) antagonist 1 exhibited a polypharmacological profile as a dual modulator of peroxisome proliferator-activated receptor (PPAR)γ/δ, we discovered a new template, 1′-homologated adenosine analogues 4a-4t, as dual PPARγ/δmodulators without AR binding. Removal of binding affinity to A3AR was achieved by 1′-homologation, and PPARγ/δdual modulation was derived from the structural similarity between the target nucleosides and PPAR modulator drug, rosiglitazone. All the final nucleosides were devoid of AR-binding affinity and exhibited high binding affinities to PPARγ/δbut lacked PPARα binding. 2-Cl derivatives exhibited dual receptor-binding affinity to PPARγ/δ, which was absent for the corresponding 2-H derivatives. 2-Propynyl substitution prevented PPARδ-binding affinity but preserved PPARγaffinity, indicating that the C2 position defines a pharmacophore for selective PPARγligand designs. PPARγ/δdual modulators functioning as both PPARγpartial agonists and PPARδantagonists promoted adiponectin production, suggesting their therapeutic potential against hypoadiponectinemia-associated cancer and metabolic diseases. © 2020 American Chemical Society. All rights reserved. | - |
dc.description.sponsorship | This work was supported by the National Research Foundation (NRF) grants (NRF - 2016R1A2B3010164, 2018R1A5A2024425, and 2019R1F1A1063905) of Korea. | - |
dc.language | en | - |
dc.publisher | American Chemical Society | - |
dc.title | Discovery and Structure-Activity Relationships of Novel Template, Truncated 1′-Homologated Adenosine Derivatives as Pure Dual PPARγ/δModulators | - |
dc.type | Article | - |
dc.relation.no | 24 | - |
dc.relation.volume | 63 | - |
dc.identifier.doi | 10.1021/acs.jmedchem.0c01874 | - |
dc.relation.page | 16012.0-16027.0 | - |
dc.relation.journal | Journal of Medicinal Chemistry | - |
dc.contributor.googleauthor | An, S. | - |
dc.contributor.googleauthor | Kim, G. | - |
dc.contributor.googleauthor | Kim, H.J. | - |
dc.contributor.googleauthor | Ahn, S. | - |
dc.contributor.googleauthor | Kim, H.Y. | - |
dc.contributor.googleauthor | Ko, H. | - |
dc.contributor.googleauthor | Hyun, Y.E. | - |
dc.contributor.googleauthor | Nguyen, M. | - |
dc.contributor.googleauthor | Jeong, J. | - |
dc.contributor.googleauthor | Liu, Z. | - |
dc.contributor.googleauthor | Han, J. | - |
dc.contributor.googleauthor | Choi, H. | - |
dc.contributor.googleauthor | Yu, J. | - |
dc.contributor.googleauthor | Kim, J.W. | - |
dc.contributor.googleauthor | Lee, H.W. | - |
dc.contributor.googleauthor | Jacobson, K.A. | - |
dc.contributor.googleauthor | Cho, W.J. | - |
dc.contributor.googleauthor | Kim, Y.-M. | - |
dc.contributor.googleauthor | Kang, K.W. | - |
dc.contributor.googleauthor | Noh, M. | - |
dc.contributor.googleauthor | Jeong, L.S. | - |
dc.sector.campus | E | - |
dc.sector.daehak | 약학대학 | - |
dc.sector.department | 약학과 | - |
dc.identifier.pid | ymikim12 | - |
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