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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2008-1-9
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pubmed:abstractText |
In an effort to obtain a MMP selective and potent inhibitor of HER-2 sheddase (ADAM-10), the P1' group of a novel class of (6S,7S)-7-[(hydroxyamino)carbonyl]-6-carboxamide-5-azaspiro[2.5]octane-5-carboxylates was attenuated and the structure-activity relationships (SAR) will be discussed. In addition, it was discovered that unconventional perturbation of the P2' moiety could confer MMP selectivity, which was hypothesized to be a manifestation of the P2' group effecting global conformational changes.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/ADAM Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/ADAM10 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Amides,
http://linkedlifedata.com/resource/pubmed/chemical/Amyloid Precursor Protein Secretases,
http://linkedlifedata.com/resource/pubmed/chemical/Aza Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Hydroxamic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Membrane Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, erbB-2,
http://linkedlifedata.com/resource/pubmed/chemical/Spiro Compounds
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BurnsDavid MDM,
pubmed-author:ChoK HKH,
pubmed-author:CovingtonMaryanne BMB,
pubmed-author:FridmanJordan SJS,
pubmed-author:FriedmanSteveS,
pubmed-author:HeChunhongC,
pubmed-author:HollisGregoryG,
pubmed-author:LiYanlongY,
pubmed-author:LiYun-LongYL,
pubmed-author:LiuXiangdongX,
pubmed-author:MarandoCindy ACA,
pubmed-author:MetcalfBrianB,
pubmed-author:NewtonRobertR,
pubmed-author:QianDing-QuanDQ,
pubmed-author:ScherlePeggyP,
pubmed-author:ShiEricE,
pubmed-author:VaddiKrisK,
pubmed-author:WassermanZelda RZR,
pubmed-author:XuMeizhongM,
pubmed-author:YangGengjieG,
pubmed-author:YaoWenqingW,
pubmed-author:YeleswaramSwamyS,
pubmed-author:ZhangColinC,
pubmed-author:ZhuoJincongJ
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
159-63
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18036818-ADAM Proteins,
pubmed-meshheading:18036818-Amides,
pubmed-meshheading:18036818-Amyloid Precursor Protein Secretases,
pubmed-meshheading:18036818-Aza Compounds,
pubmed-meshheading:18036818-Drug Design,
pubmed-meshheading:18036818-Hydroxamic Acids,
pubmed-meshheading:18036818-Membrane Proteins,
pubmed-meshheading:18036818-Protein Kinase Inhibitors,
pubmed-meshheading:18036818-Protein Structure, Tertiary,
pubmed-meshheading:18036818-Receptor, erbB-2,
pubmed-meshheading:18036818-Spiro Compounds,
pubmed-meshheading:18036818-Structure-Activity Relationship,
pubmed-meshheading:18036818-Substrate Specificity
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pubmed:year |
2008
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pubmed:articleTitle |
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
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pubmed:affiliation |
Incyte Corporation, Department of Medicinal Chemistry, Wilmington, DE 19880, USA. wyao@incyte.com
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pubmed:publicationType |
Journal Article
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