Source:http://linkedlifedata.com/resource/pubmed/id/16854083
Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
15
|
| pubmed:dateCreated |
2006-7-20
|
| pubmed:abstractText |
A series of Gly-neurotensin(8-13) analogues modified at the N-terminus by acyclic tetraamines (Demotensin 1-4) were obtained by solid-phase peptide synthesis techniques. Strategic replacement of amino acids and/or reduction of sensitive peptide bonds were performed to enhance conjugate resistance against proteolytic enzymes. During 99mTc-labeling, single species radiopeptides, [99mTc]Demotensin 1-4, were easily obtained in high yields and typical specific activities of 1 Ci/micromol. Peptide conjugates displayed a high affinity binding to the human neurotensin subtype 1 receptor (NTS1-R) expressed in colon adenocarcinoma HT-29 or WiDr cells and/or in human tumor sections. [99mTc]Demotensin 1-4 internalized very rapidly in HT-29 or WiDr cells by a NTS1-R-mediated process. [99mTc]Demotensin 3 and 4, which remained stable during 1 h incubation in murine plasma, were selectively studied in nude mice bearing human HT-29 and WiDr xenografts. After injection, [99mTc]Demotensin 3 and 4 effectively and specifically localized in the experimental tumors and were rapidly excreted via the kidneys into the urine, exhibiting overall biodistribution patterns favorable for NTS1-R-targeted tumor imaging in man.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Neurotensin,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Organotechnetium Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neurotensin,
http://linkedlifedata.com/resource/pubmed/chemical/neurotensin type 1 receptor
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jul
|
| pubmed:issn |
0022-2623
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
27
|
| pubmed:volume |
49
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
4767-76
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:16854083-Animals,
pubmed-meshheading:16854083-Carcinoma, Pancreatic Ductal,
pubmed-meshheading:16854083-Cell Line, Tumor,
pubmed-meshheading:16854083-Drug Stability,
pubmed-meshheading:16854083-Female,
pubmed-meshheading:16854083-Humans,
pubmed-meshheading:16854083-Male,
pubmed-meshheading:16854083-Mice,
pubmed-meshheading:16854083-Mice, Nude,
pubmed-meshheading:16854083-Neoplasms,
pubmed-meshheading:16854083-Neurotensin,
pubmed-meshheading:16854083-Oligopeptides,
pubmed-meshheading:16854083-Organotechnetium Compounds,
pubmed-meshheading:16854083-Pancreatic Neoplasms,
pubmed-meshheading:16854083-Radiopharmaceuticals,
pubmed-meshheading:16854083-Receptors, Neurotensin,
pubmed-meshheading:16854083-Structure-Activity Relationship,
pubmed-meshheading:16854083-Tissue Distribution,
pubmed-meshheading:16854083-Transplantation, Heterologous
|
| pubmed:year |
2006
|
| pubmed:articleTitle |
Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc.
|
| pubmed:affiliation |
Institute of Radioisotopes - Radiodiagnostic Products, National Center for Scientific Research Demokritos, 15310 Athens, Greece.
|
| pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
|