Source:http://linkedlifedata.com/resource/pubmed/id/19854643
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
23
|
pubmed:dateCreated |
2009-11-5
|
pubmed:abstractText |
We describe herein the synthesis and characterization of a new class of histone deacetylase (HDAC) inhibitors derived from conjugation of a suberoylanilide hydroxamic acid-like aliphatic-hydroxamate pharmacophore to a nuclear localization signal peptide. We found that these conjugates inhibited the histone deacetylase activities of HDACs 1, 2, 6, and 8 in a manner similar to suberoylanilide hydroxamic acid (SAHA). Notably, compound 7b showed a threefold improvement in HDAC 1/2 inhibition, a threefold increase in HDAC 6 selectivity and a twofold increase in HDAC 8 selectivity when compared to SAHA.
|
pubmed:grant | |
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Histone Deacetylase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Histone Deacetylases,
http://linkedlifedata.com/resource/pubmed/chemical/Hydroxamic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Nuclear Localization Signals
|
pubmed:status |
MEDLINE
|
pubmed:month |
Dec
|
pubmed:issn |
1464-3405
|
pubmed:author | |
pubmed:issnType |
Electronic
|
pubmed:day |
1
|
pubmed:volume |
19
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
6588-90
|
pubmed:dateRevised |
2011-6-1
|
pubmed:meshHeading |
pubmed-meshheading:19854643-Drug Design,
pubmed-meshheading:19854643-Histone Deacetylase Inhibitors,
pubmed-meshheading:19854643-Histone Deacetylases,
pubmed-meshheading:19854643-Hydroxamic Acids,
pubmed-meshheading:19854643-Molecular Conformation,
pubmed-meshheading:19854643-Nuclear Localization Signals,
pubmed-meshheading:19854643-Stereoisomerism,
pubmed-meshheading:19854643-Structure-Activity Relationship
|
pubmed:year |
2009
|
pubmed:articleTitle |
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.
|
pubmed:affiliation |
School of Chemistry and Biochemistry, Parker H Petit Institute for Bioengineering and Bioscience, Georgia Institute of Technology, Atlanta, GA 30332-0400, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
|