Linked Life Data

19303174

Source:http://linkedlifedata.com/resource/pubmed/id/19303174

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
2009-7-20
pubmed:abstractText
We report the design of a new ligand of integrins that might be used for the molecular imaging of tumor neoangiogenesis. For this purpose, we designed a modified RGD tripeptide bearing a N-terminal N-bis(thioethyl)glycinate (NS(2)) motif and a thioethyl moiety at the C-terminus. Simultaneous coordination of an oxorhenium core by the NS(2) and thioethyl moieties led to peptide cyclization and gave the corresponding monomers 13a and b (major isomer) resulting from the syn/anti-isomerism, along with dimers' species 16a and b. Cyclometallated peptide 13b showed the most promising activity with an IC(50) of 86 nM for integrin alpha(V)beta(3) whereas it binds integrin alpha(IIb)beta(3) with an affinity lower by an order of magnitude. Labeling with [(99m)Tc]oxotechnetium gluconate led exclusively to complex 17, the equivalent of compound 13b, which displayed satisfactory stabilities in mice plasma and towards glutathione.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
1768-3254
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
44
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3394-401
pubmed:meshHeading
pubmed:year
2009
pubmed:articleTitle
Synthesis and biochemical evaluation of a cyclic RGD oxorhenium complex as new ligand of alphaVbeta3 integrin.
pubmed:affiliation
CEA/Saclay, iBiTec-S/SIMOPRO, Bâtiment 152, 91191 Gif-sur-Yvette, France.
pubmed:publicationType
Journal Article