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α-Arylidene diacylglycerol-lactones (DAG-Lactones) as selective ras guanine-releasing protein 3 (RasGRP3) ligands : alpha-Arylidene diacylglycerol-lactones (DAG-Lactones) as selective ras guanine-releasing protein 3 (RasGRP3) ligands
DC Field | Value | Language |
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dc.contributor.author | Ann, Jihyae | - |
dc.contributor.author | Czikora, Agnes | - |
dc.contributor.author | Saini, Amandeep S. | - |
dc.contributor.author | Zhou, Xiaoling | - |
dc.contributor.author | Mitchell, Gary A. | - |
dc.contributor.author | Lewin, Nancy E. | - |
dc.contributor.author | Peach, Megan L. | - |
dc.contributor.author | Blumberg, Peter M. | - |
dc.contributor.author | Lee, Jeewoo | - |
dc.creator | 이지우 | - |
dc.date.accessioned | 2019-04-25T02:06:44Z | - |
dc.date.available | 2020-04-05T02:06:44Z | - |
dc.date.created | 2019-06-27 | - |
dc.date.issued | 2018-07-26 | - |
dc.identifier.citation | Journal of Medicinal Chemistry, Vol.61 No.14, pp.6261-6276 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | https://hdl.handle.net/10371/150211 | - |
dc.description.abstract | Diacylglycerol-lactones have proven to be a powerful template for the design of potent ligands targeting CI domains, the recognition motif for the cellular second messenger diacylglycerol. A major objective has been to better understand the structure activity relations distinguishing the seven families of signaling proteins that contain such domains, of which the protein kinase C (PKC) and RasGRP families are of particular interest. Here, we synthesize a series of aryl- and alkyl-substituted diacylglycerol-lactones and probe their relative selectivities for RasGRP3 versus PKC. Compound 96 showed 73-fold selectivity relative to PKC alpha 45 and 45-fold selectivity relative to PKC epsilon for in vitro binding activity. Likewise, in intact cells, compound 96 induced Ras activation, a downstream response to RasGRP stimulation, with 8-29 fold selectivity relative to PKC delta S299 phosphorylation, a measure of PKC delta stimulation. | - |
dc.language | 영어 | - |
dc.language.iso | en | en |
dc.publisher | American Chemical Society | - |
dc.title | α-Arylidene diacylglycerol-lactones (DAG-Lactones) as selective ras guanine-releasing protein 3 (RasGRP3) ligands | - |
dc.title.alternative | alpha-Arylidene diacylglycerol-lactones (DAG-Lactones) as selective ras guanine-releasing protein 3 (RasGRP3) ligands | - |
dc.type | Article | - |
dc.identifier.doi | 10.1021/acs.jmedchem.8b00661 | - |
dc.citation.journaltitle | Journal of Medicinal Chemistry | - |
dc.identifier.wosid | 000440521300030 | - |
dc.identifier.scopusid | 2-s2.0-85048144752 | - |
dc.description.srnd | OAIID:RECH_ACHV_DSTSH_NO:T201824369 | - |
dc.description.srnd | RECH_ACHV_FG:RR00200001 | - |
dc.description.srnd | ADJUST_YN: | - |
dc.description.srnd | EMP_ID:A003772 | - |
dc.description.srnd | CITE_RATE:6.253 | - |
dc.description.srnd | DEPT_NM:약학과 | - |
dc.description.srnd | EMAIL:jeewoo@snu.ac.kr | - |
dc.description.srnd | SCOPUS_YN:Y | - |
dc.citation.endpage | 6276 | - |
dc.citation.number | 14 | - |
dc.citation.startpage | 6261 | - |
dc.citation.volume | 61 | - |
dc.description.isOpenAccess | N | - |
dc.contributor.affiliatedAuthor | Lee, Jeewoo | - |
dc.identifier.srnd | T201824369 | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | CONFORMATIONALLY CONSTRAINED ANALOGS | - |
dc.subject.keywordPlus | KINASE-C | - |
dc.subject.keywordPlus | PHORBOL ESTER | - |
dc.subject.keywordPlus | BINDING | - |
dc.subject.keywordPlus | ACTIVATORS | - |
dc.subject.keywordPlus | REVEALS | - |
dc.subject.keywordPlus | DOMAINS | - |
dc.subject.keywordPlus | DELTA | - |
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