Linked Life Data

18158948

Source:http://linkedlifedata.com/resource/pubmed/id/18158948

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2007-12-26
pubmed:abstractText
Melanoma primary tumors can be, in most cases, removed surgically, whereas there is no satisfactory treatment for metastatic melanoma, being almost always lethal at this stage. Therefore, early detection of primary melanoma tumors is essential. The finding that melanocortin-1 receptor (MC1R) is overexpressed in isolated melanoma cells and melanoma tissues led to the radiolabeling of several alpha-melanocyte-stimulating hormone (alpha-MSH) analogs for early detection and treatment of melanoma. We have coupled the alpha-MSH analog Ac-Nle-Asp-His-d-Phe-Arg-Trp-Gly-Lys-NH(2), through the epsilon-amino group of Lys(11), to a pyrazolyl-containing chelator (pz). The resulting pz-alpha-MSH analog reacted with the fac-[(99m)Tc(CO)(3)](+) moiety, giving [Ac-Nle(4),Asp(5),d-Phe(7),Lys(11)(pz-(99m)Tc(CO)(3))]alpha-MSH(4-11) in high yield, high specific activity and high radiochemical purity. This radioconjugate, which presents remarkable stability in vitro, exhibited time- and temperature-dependent internalization (4 h at 37 degrees C; 56.7% maximum internalization) and high cellular retention (only 38% was released from the cell after 5 h) in murine melanoma B16F1 cells. A significant tumor uptake [4.2+/-0.9%ID/g, at 4 h postinjection (p.i.)] was also obtained in melanoma-bearing C57BL6 mice. The in vivo affinity and specificity of the radioconjugate to MC1R were demonstrated by receptor-blocking studies with the potent NDP-MSH agonist (63.5% reduction in tumor uptake at 4 h p.i.).
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0969-8051
pubmed:author
pubmed:issnType
Print
pubmed:volume
35
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
91-9
pubmed:meshHeading
pubmed:year
2008
pubmed:articleTitle
A (99m)Tc(CO)(3)-labeled pyrazolyl-alpha-melanocyte-stimulating hormone analog conjugate for melanoma targeting.
pubmed:affiliation
Departamento de Química, ITN, Estrada Nacional 10, 2686-953 Sacavém, Portugal.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't