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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2008-2-5
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pubmed:abstractText |
We report herein the initial exploration of novel selective HDAC1/HDAC2 inhibitors (SHI-1:2). Optimized SHI-1:2 structures exhibit enhanced intrinsic activity against HDAC1 and HDAC2, and are greater than 100-fold selective versus other HDACs, including HDAC3. Based on the SAR of these agents and our current understanding of the HDAC active site, we postulate that the SHI-1:2 extend the existing HDAC inhibitor pharmacophore to include an internal binding domain.
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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 |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:ChakravartyPrasun KPK,
pubmed-author:ChenardMelissaM,
pubmed-author:CloseJoshuaJ,
pubmed-author:CruzJonathan CJC,
pubmed-author:DahlbergWilliam KWK,
pubmed-author:FlemingJudithJ,
pubmed-author:HamblettChristopher LCL,
pubmed-author:HamillJulie EJE,
pubmed-author:HarringtonPaulP,
pubmed-author:HarschAndreasA,
pubmed-author:HeidebrechtRichardR,
pubmed-author:HughesBethanyB,
pubmed-author:KenificCandia MCM,
pubmed-author:KralAstrid MAM,
pubmed-author:MeinkePeter TPT,
pubmed-author:MethotJoey LJL,
pubmed-author:MiddletonRichard ERE,
pubmed-author:MillerThomas ATA,
pubmed-author:ObiG OGO,
pubmed-author:OzerovaNicoleN,
pubmed-author:SecristJ PaulJP,
pubmed-author:SlomanDavid LDL,
pubmed-author:StantonMatthew GMG,
pubmed-author:SzewczakAlexander AAA,
pubmed-author:TyagarajanSriramS,
pubmed-author:WitterDavid JDJ
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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 |
973-8
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:18182289-Benzene Derivatives,
pubmed-meshheading:18182289-Binding Sites,
pubmed-meshheading:18182289-Histone Deacetylase 1,
pubmed-meshheading:18182289-Histone Deacetylase 2,
pubmed-meshheading:18182289-Histone Deacetylase Inhibitors,
pubmed-meshheading:18182289-Histone Deacetylases,
pubmed-meshheading:18182289-Humans,
pubmed-meshheading:18182289-Models, Molecular,
pubmed-meshheading:18182289-Molecular Structure,
pubmed-meshheading:18182289-Protein Isoforms,
pubmed-meshheading:18182289-Repressor Proteins,
pubmed-meshheading:18182289-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).
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pubmed:affiliation |
Department of Drug Design and Optimization, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. joey_methot@merck.com
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pubmed:publicationType |
Journal Article
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