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rdf:type |
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|
lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
2009-10-26
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pubmed:abstractText |
Design and synthesis of an HDAC inhibitor and its merger with three tubulin binders to create releasable conjugate compounds is described. The biological evaluation includes: (a) in vitro reactivity with glutathione, (b) antiproliferative activity, (c) cell cycle analysis and (d) quantification of protein acetylation. The cellular pharmacology study indicated that the HDAC-inhibitor-drug conjugates retained antimitotic and proapoptotic activity with a reduced potency.
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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 |
Nov
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pubmed:issn |
1464-3405
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pubmed:author |
|
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6358-63
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pubmed:meshHeading |
pubmed-meshheading:19833515-Acetylation,
pubmed-meshheading:19833515-Antineoplastic Agents,
pubmed-meshheading:19833515-Cell Cycle,
pubmed-meshheading:19833515-Drug Design,
pubmed-meshheading:19833515-Glutathione,
pubmed-meshheading:19833515-HeLa Cells,
pubmed-meshheading:19833515-Histone Deacetylase 2,
pubmed-meshheading:19833515-Histone Deacetylases,
pubmed-meshheading:19833515-Humans,
pubmed-meshheading:19833515-Microtubule-Associated Proteins,
pubmed-meshheading:19833515-Microtubules,
pubmed-meshheading:19833515-Protein Processing, Post-Translational,
pubmed-meshheading:19833515-Protein Structure, Tertiary,
pubmed-meshheading:19833515-Structure-Activity Relationship,
pubmed-meshheading:19833515-Tubulin
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pubmed:year |
2009
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pubmed:articleTitle |
Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds.
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pubmed:affiliation |
Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, Italy. Daniele.Passarella@unimi.it
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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