|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
21
|
|
pubmed:dateCreated |
2009-11-5
|
|
pubmed:abstractText |
A series of mitoxantrone (MTX) analogues have been designed, synthesized, and evaluated for binding to and stabilizing a stem-loop structure that serves as a splicing regulatory element in the pre-mRNA of tau, which is involved in Alzheimer's and other neurodegenerative diseases. Several compounds showed significantly improved binding activity relative to the original screening hit mitoxantrone. These findings establish essential structure-activity relationships to further optimize the activity of this promising class of compounds.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Nov
|
|
pubmed:issn |
1520-4804
|
|
pubmed:author |
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
12
|
|
pubmed:volume |
52
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
6523-6
|
|
pubmed:meshHeading |
pubmed-meshheading:19839622-Anthraquinones,
pubmed-meshheading:19839622-Binding, Competitive,
pubmed-meshheading:19839622-Ligands,
pubmed-meshheading:19839622-Mitoxantrone,
pubmed-meshheading:19839622-Models, Molecular,
pubmed-meshheading:19839622-Polyamines,
pubmed-meshheading:19839622-RNA, Messenger,
pubmed-meshheading:19839622-RNA Precursors,
pubmed-meshheading:19839622-RNA Splicing,
pubmed-meshheading:19839622-Regulatory Elements, Transcriptional,
pubmed-meshheading:19839622-Structure-Activity Relationship,
pubmed-meshheading:19839622-tau Proteins
|
|
pubmed:year |
2009
|
|
pubmed:articleTitle |
Mitoxantrone analogues as ligands for a stem-loop structure of tau pre-mRNA.
|
|
pubmed:affiliation |
Center for Neurologic Diseases, Brigham and Women's Hospital and Harvard Medical School,H.I.M. 754, Boston, Massachusetts 02115, USA.
|
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|
