Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 최선 | * |
dc.contributor.author | 이윤지 | * |
dc.date.accessioned | 2021-02-25T16:31:47Z | - |
dc.date.available | 2021-02-25T16:31:47Z | - |
dc.date.issued | 2021 | * |
dc.identifier.issn | 0022-2623 | * |
dc.identifier.issn | 1520-4804 | * |
dc.identifier.other | OAK-28893 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/257149 | - |
dc.description.abstract | Among a series of benzopyridone-based scaffolds investigated as human transient receptor potential vanilloid 1 (TRPV1) ligands, two isomeric benzopyridone scaffolds demonstrated a consistent and distinctive functional profile in which 2-oxo-1,2-dihydroquinolin-5-yl analogues (e.g., 2) displayed high affinity and potent antagonism, whereas 1-oxo-1,2-dihydroisoquinolin-5-yl analogues (e.g., 3) showed full agonism with high potency. Our computational models provide insight into the agonist-antagonist boundary of the analogues suggesting that the Arg557 residue in the S4-S5 linker might be important for sensing the agonist binding and transmitting signals. These results provide structural insights into the TRPV1 and the protein-ligand interactions at a molecular level. | * |
dc.language | English | * |
dc.publisher | AMER CHEMICAL SOC | * |
dc.title | Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift | * |
dc.type | Article | * |
dc.relation.issue | 1 | * |
dc.relation.volume | 64 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 370 | * |
dc.relation.lastpage | 384 | * |
dc.relation.journaltitle | JOURNAL OF MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1021/acs.jmedchem.0c00982 | * |
dc.identifier.wosid | WOS:000611409600018 | * |
dc.identifier.scopusid | 2-s2.0-85100070142 | * |
dc.author.google | Thorat, Shivaji A. | * |
dc.author.google | Lee, Yoonji | * |
dc.author.google | Jung, Aeran | * |
dc.author.google | Ann, Jihyae | * |
dc.author.google | Ahn, Songyeon | * |
dc.author.google | Baek, Jisoo | * |
dc.author.google | Zuo, Dongxu | * |
dc.author.google | Do, Nayeon | * |
dc.author.google | Jeong, Jin Ju | * |
dc.author.google | Blumberg, Peter M. | * |
dc.author.google | Esch, Timothy E. | * |
dc.author.google | Turcios, Noe A. | * |
dc.author.google | Pearce, Larry, V | * |
dc.author.google | Ha, Hee-Jin | * |
dc.author.google | Yoo, Young Dong | * |
dc.author.google | Hong, Sunhye | * |
dc.author.google | Choi, Sun | * |
dc.author.google | Lee, Jeewoo | * |
dc.contributor.scopusid | 최선(8659831000) | * |
dc.contributor.scopusid | 이윤지(16836651600) | * |
dc.date.modifydate | 20240305081003 | * |