rdf:type |
|
lifeskim:mentions |
umls-concept:C0002068,
umls-concept:C0012512,
umls-concept:C0205369,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243071,
umls-concept:C0441587,
umls-concept:C0762772,
umls-concept:C1332823,
umls-concept:C1709743,
umls-concept:C1883254,
umls-concept:C1999216
|
pubmed:issue |
6
|
pubmed:dateCreated |
2002-4-17
|
pubmed:abstractText |
A 14-residue peptide, T140, strongly inhibits the T-cell line-tropic HIV-1 (X4-HIV-1) infection, since this peptide functions as a specific antagonist against a chemokine receptor, CXCR4. T140 takes an antiparallel beta-sheet structure with a type II' beta-turn. In the present paper, we have designed and synthesized several T140 analogues, in which an (E)-alkene dipeptide isostere was inserted into the type II' beta-turn moiety, as a bridging study to develop nonpeptidic CXCR4 inhibitors. It has been proven that the turn region of T140 can be replaced by the above surrogate with the maintenance of strong anti-HIV activity.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
0960-894X
|
pubmed:author |
pubmed-author:FujiiNobutakaN,
pubmed-author:HiramatsuKenichiK,
pubmed-author:KurodaYoshihiroY,
pubmed-author:MiyamotoKazuhideK,
pubmed-author:NakagawaTerumichiT,
pubmed-author:NakashimaHidekiH,
pubmed-author:OishiShinyaS,
pubmed-author:OmagariAkaneA,
pubmed-author:OtakaAkiraA,
pubmed-author:TamamuraHirokazuH,
pubmed-author:YamamotoNaokiN
|
pubmed:issnType |
Print
|
pubmed:day |
25
|
pubmed:volume |
12
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
923-8
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:11958995-Anti-HIV Agents,
pubmed-meshheading:11958995-Calcium Signaling,
pubmed-meshheading:11958995-Cell Division,
pubmed-meshheading:11958995-Dipeptides,
pubmed-meshheading:11958995-HIV-1,
pubmed-meshheading:11958995-Humans,
pubmed-meshheading:11958995-Inhibitory Concentration 50,
pubmed-meshheading:11958995-Microbial Sensitivity Tests,
pubmed-meshheading:11958995-Models, Molecular,
pubmed-meshheading:11958995-Oligopeptides,
pubmed-meshheading:11958995-Protein Structure, Secondary,
pubmed-meshheading:11958995-Receptors, CXCR4,
pubmed-meshheading:11958995-Tumor Cells, Cultured
|
pubmed:year |
2002
|
pubmed:articleTitle |
Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety.
|
pubmed:affiliation |
Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, 606-8501, Kyoto, Japan. tamamura@pharm.kyoto-u.ac.jp
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|