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SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists
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| DC Field | Value | Language |
|---|---|---|
| dc.contributor.author | Yoon, Dong-Oh | - |
| dc.contributor.author | Zhao, Xiaodi | - |
| dc.contributor.author | Son, Dohyun | - |
| dc.contributor.author | Han, Jung Tae | - |
| dc.contributor.author | Yun, Jaesook | - |
| dc.contributor.author | Shin, Dongyun | - |
| dc.contributor.author | Park, Hyun-Ju | - |
| dc.date.available | 2020-02-27T16:42:07Z | - |
| dc.date.created | 2020-02-06 | - |
| dc.date.issued | 2017-12 | - |
| dc.identifier.issn | 1948-5875 | - |
| dc.identifier.uri | https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/5432 | - |
| dc.description.abstract | G-protein coupled receptor 40 (GPR40) has been considered to be an attractive drug target for the treatment of type 2 diabetes because of its role in free fatty acids-mediated enhancement of glucose-stimulated insulin secretion (GSIS) from pancreatic beta-cells. A series of indole-5-propanoic acid compounds were synthesized, and their GPR40 agonistic activities were evaluated by nuclear factor of activated T-cells reporter assay and GSIS assay in the MIN-6 insulinoma cells. Three compounds, 8h (EC50 = 58.6 nM), 8i (EC50 = 37.8 nM), and 8o (EC50 = 9.4 nM), were identified as potent GPR40 agonists with good GSIS effects. | - |
| dc.language | 영어 | - |
| dc.language.iso | en | - |
| dc.publisher | AMER CHEMICAL SOC | - |
| dc.relation.isPartOf | ACS MEDICINAL CHEMISTRY LETTERS | - |
| dc.subject | PANCREATIC BETA-CELLS | - |
| dc.subject | 1 FFA1/GPR40 AGONIST | - |
| dc.subject | FREE FATTY-ACIDS | - |
| dc.subject | INSULIN-SECRETION | - |
| dc.subject | DIABETES-MELLITUS | - |
| dc.subject | PI INTERACTIONS | - |
| dc.subject | IN-VITRO | - |
| dc.subject | DISCOVERY | - |
| dc.subject | POTENT | - |
| dc.subject | TAK-875 | - |
| dc.title | SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists | - |
| dc.type | Article | - |
| dc.type.rims | ART | - |
| dc.description.journalClass | 1 | - |
| dc.identifier.wosid | 000418393700024 | - |
| dc.identifier.doi | 10.1021/acsmedchemlett.7b00460 | - |
| dc.identifier.bibliographicCitation | ACS MEDICINAL CHEMISTRY LETTERS, v.8, no.12, pp.1336 - 1340 | - |
| dc.identifier.scopusid | 2-s2.0-85038365165 | - |
| dc.citation.endPage | 1340 | - |
| dc.citation.startPage | 1336 | - |
| dc.citation.title | ACS MEDICINAL CHEMISTRY LETTERS | - |
| dc.citation.volume | 8 | - |
| dc.citation.number | 12 | - |
| dc.contributor.affiliatedAuthor | Shin, Dongyun | - |
| dc.type.docType | Article | - |
| dc.subject.keywordAuthor | GPR40 agonists | - |
| dc.subject.keywordAuthor | indole-5-propanoic acid | - |
| dc.subject.keywordAuthor | NFAT reporter assay | - |
| dc.subject.keywordAuthor | glucose-stimulated insulin secretion (GSIS) | - |
| dc.subject.keywordPlus | PANCREATIC BETA-CELLS | - |
| dc.subject.keywordPlus | 1 FFA1/GPR40 AGONIST | - |
| dc.subject.keywordPlus | FREE FATTY-ACIDS | - |
| dc.subject.keywordPlus | INSULIN-SECRETION | - |
| dc.subject.keywordPlus | DIABETES-MELLITUS | - |
| dc.subject.keywordPlus | PI INTERACTIONS | - |
| dc.subject.keywordPlus | IN-VITRO | - |
| dc.subject.keywordPlus | DISCOVERY | - |
| dc.subject.keywordPlus | POTENT | - |
| dc.subject.keywordPlus | TAK-875 | - |
| dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
| dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
| dc.description.journalRegisteredClass | scie | - |
| dc.description.journalRegisteredClass | scopus | - |
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Related Researcher
- Shin, Dong Yun
- Pharmacy (Dept.of Pharmacy)