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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2010-2-22
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pubmed:abstractText |
Valosin-containing protein (VCP; also known as p97) is a member of the AAA ATPase family with a central role in the ubiquitin-degradation of misfolded proteins. VCP also exhibits antiapoptotic function and metastasis via activation of nuclear factor kappa-B signaling pathway. We have discovered that 2-anilino-4-aryl-1,3-thiazoles are potent drug-like inhibitors of this enzyme. The identified compounds show low nanomolar VCP potency, demonstrate SAR trends, and show activity in a mechanism based cellular assay. This series of compounds represents the first steps towards a novel, small molecule VCP inhibitor as a cancer therapeutic.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BursavichMatthew GMG,
pubmed-author:CimboraDaniel MDM,
pubmed-author:DavisThaylonT,
pubmed-author:GaoZhong-HuaZH,
pubmed-author:OstaninKirillK,
pubmed-author:ParkerDaniel PDP,
pubmed-author:PetersonAshleyA,
pubmed-author:RichardsBurtB,
pubmed-author:RobinsonRosannR,
pubmed-author:WillardsenJ AdamJA,
pubmed-author:ZhuJu-FenJF
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1677-9
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pubmed:meshHeading |
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pubmed:year |
2010
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pubmed:articleTitle |
2-Anilino-4-aryl-1,3-thiazole inhibitors of valosin-containing protein (VCP or p97).
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pubmed:affiliation |
Medicinal Chemistry, Myriad Pharmaceuticals, Inc., 305 South Chipeta Way, Salt Lake City, UT 84108, United States. Matthew.Bursavich@myriadpharma.com
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pubmed:publicationType |
Journal Article
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