rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
15
|
pubmed:dateCreated |
2004-6-30
|
pubmed:abstractText |
Structure-based-design studies, with the crystal structure of the HOXB1-PBX1/DNA transcription factor complex, were used to identify 1,4-disubstituted naphthalenes as potential antagonists. An initial library of 32 analogs was synthesized, two of which were found to be more potent than the reported activity for a 12 amino acid peptide antagonist. Antagonists were also identified of the related BRN1/DNA and BRN2/DNA transcription factor complexes indicating that a 1,4-disubstituted naphthalene may be a privileged scaffold for preparing screening libraries targeting this family of transcription factor complexes.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Aug
|
pubmed:issn |
0960-894X
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
2
|
pubmed:volume |
14
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
3875-9
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:15225688-Crystallography, X-Ray,
pubmed-meshheading:15225688-DNA,
pubmed-meshheading:15225688-DNA-Binding Proteins,
pubmed-meshheading:15225688-Homeodomain Proteins,
pubmed-meshheading:15225688-Humans,
pubmed-meshheading:15225688-Kinetics,
pubmed-meshheading:15225688-Models, Molecular,
pubmed-meshheading:15225688-Naphthalenes,
pubmed-meshheading:15225688-Proto-Oncogene Proteins,
pubmed-meshheading:15225688-Transcription Factors
|
pubmed:year |
2004
|
pubmed:articleTitle |
Privileged scaffolds for blocking protein-protein interactions: 1,4-disubstituted naphthalene antagonists of transcription factor complex HOX-PBX/DNA.
|
pubmed:affiliation |
Department of Chemistry, University at Buffalo, The State University of New York, Buffalo, NY 14260-3000, USA.
|
pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
|