https://scholars.lib.ntu.edu.tw/handle/123456789/568504
DC 欄位 | 值 | 語言 |
---|---|---|
dc.contributor.author | Chen K.-F. | en_US |
dc.contributor.author | Tai W.-T. | en_US |
dc.contributor.author | Hsu C.-Y. | en_US |
dc.contributor.author | Huang J.-W. | en_US |
dc.contributor.author | Liu C.-Y. | en_US |
dc.contributor.author | PEI-JER CHEN | en_US |
dc.contributor.author | Kim I. | en_US |
dc.contributor.author | Shiau C.-W. | en_US |
dc.date.accessioned | 2021-07-03T03:34:30Z | - |
dc.date.available | 2021-07-03T03:34:30Z | - |
dc.date.issued | 2012 | - |
dc.identifier.issn | 0223-5234 | - |
dc.identifier.uri | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84984563938&doi=10.1016%2fj.ejmech.2012.07.023&partnerID=40&md5=375eeb9386bb4486100a32aacfbd35fc | - |
dc.identifier.uri | https://scholars.lib.ntu.edu.tw/handle/123456789/568504 | - |
dc.description.abstract | Previously, we demonstrated that the multiple kinase inhibitor sorafenib mediates the repression of phospho-STAT3 in hepatocellular carcinoma cells. In this study, we used this kinase-independent mechanism as a molecular basis to use sorafenib as scaffold to develop a novel class of SHP-1-activating agents. The proof of principle of this premise was provided by SC-1, which on replacement of N-methylpicolinamide by a phenylcyano group showed abolished kinase activity while retaining phospho-STAT3 repressive activity. Structural optimization of SC-1 led to compound 6, which repressed phospho-STAT3 through SHP-1 activation and inhibited PLC5 cell proliferation at sub-micromolar potency. In light of the pivotal role of phospho-STAT3 in promoting tumorigenesis and drug resistance, this novel SHP-1-activating agent may have therapeutic relevance in cancer therapy. ? 2012 Elsevier Masson SAS. All rights reserved. | - |
dc.publisher | Elsevier Masson SAS | - |
dc.relation.ispartof | European Journal of Medicinal Chemistry | - |
dc.subject | HCC; SHP-1; Sorafenib; STAT3 | - |
dc.subject.classification | [SDGs]SDG3 | - |
dc.subject.other | n methylpicolinamide; phenyl group; phosphotransferase; picolinamide; protein tyrosine phosphatase SHP 1; sc 1; sorafenib; STAT3 protein; unclassified drug; animal cell; animal experiment; animal model; article; carcinogenesis; carcinoma cell; cell proliferation; cell viability; controlled study; drug potency; enzyme activation; enzyme activity; enzyme mechanism; enzyme repression; human; human cell; liver cell carcinoma; male; mouse; nonhuman; Western blotting | - |
dc.title | Blockade of STAT3 activation by sorafenib derivatives through enhancing SHP-1 phosphatase activity | en_US |
dc.type | journal article | en |
dc.identifier.doi | 10.1016/j.ejmech.2012.07.023 | - |
dc.identifier.pmid | 22871485 | - |
dc.identifier.scopus | 2-s2.0-84984563938 | - |
dc.relation.pages | 220-227 | - |
dc.relation.journalvolume | 55 | - |
item.fulltext | no fulltext | - |
item.openairetype | journal article | - |
item.openairecristype | http://purl.org/coar/resource_type/c_6501 | - |
item.grantfulltext | none | - |
item.cerifentitytype | Publications | - |
crisitem.author.dept | Clinical Medicine | - |
crisitem.author.orcid | 0000-0001-8316-3785 | - |
crisitem.author.parentorg | College of Medicine | - |
顯示於: | 臨床醫學研究所 |
在 IR 系統中的文件,除了特別指名其著作權條款之外,均受到著作權保護,並且保留所有的權利。