Source:http://linkedlifedata.com/resource/pubmed/id/16287254
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
|
| pubmed:dateCreated |
2005-11-18
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| pubmed:abstractText |
Affibody molecules are a new class of small phage-display selected proteins using a scaffold domain of the bacterial receptor protein A. They can be selected for specific binding to a large variety of protein targets. An affibody molecule binding with high affinity to a tumor antigen HER2 was recently developed for radionuclide diagnostics and therapy in vivo. The use of the positron-emitting nuclide (76)Br (T(1/2) = 16.2 h) could improve the sensitivity of detection of HER2-expressing tumors. A site-specific radiobromination of a cysteine-containing variant of the anti-HER2 affibody, (Z(HER2:4))(2)-Cys, using ((4-hydroxyphenyl)ethyl)maleimide (HPEM), was evaluated in this study. It was found that HPEM can be radiobrominated with an efficiency of 83 +/- 0.4% and thereafter coupled to freshly reduced affibody with a yield of 65.3 +/- 3.9%. A "one-pot" labeling enabled the radiochemical purity of the conjugate to exceed 97%. The label was stable against challenge with large excess of nonlabeled bromide and in a high molar strength solution. In vitro cell tests demonstrated that radiobrominated affibody binds specifically to the HER2-expressing cell-line, SK-OV-3. Biodistribution studies in nude mice bearing SK-OV-3 xenografts have shown tumor accumulation of 4.8 +/- 2.2% IA/g and good tumor-to-normal tissue ratios.
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| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antigens, Neoplasm,
http://linkedlifedata.com/resource/pubmed/chemical/Bromine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Maleimides,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Library,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Radiopharmaceuticals,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, erbB-2,
http://linkedlifedata.com/resource/pubmed/chemical/Staphylococcal Protein A
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| pubmed:status |
MEDLINE
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| pubmed:issn |
1043-1802
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| pubmed:author | |
| pubmed:issnType |
Print
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| pubmed:volume |
16
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| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1547-55
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| pubmed:dateRevised |
2009-11-19
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| pubmed:meshHeading |
pubmed-meshheading:16287254-Animals,
pubmed-meshheading:16287254-Antigens, Neoplasm,
pubmed-meshheading:16287254-Binding Sites,
pubmed-meshheading:16287254-Bromine Radioisotopes,
pubmed-meshheading:16287254-Cell Line, Tumor,
pubmed-meshheading:16287254-Humans,
pubmed-meshheading:16287254-Maleimides,
pubmed-meshheading:16287254-Mice,
pubmed-meshheading:16287254-Mice, Nude,
pubmed-meshheading:16287254-Neoplasms, Experimental,
pubmed-meshheading:16287254-Peptide Library,
pubmed-meshheading:16287254-Peptides,
pubmed-meshheading:16287254-Protein Interaction Mapping,
pubmed-meshheading:16287254-Radiopharmaceuticals,
pubmed-meshheading:16287254-Receptor, erbB-2,
pubmed-meshheading:16287254-Staphylococcal Protein A,
pubmed-meshheading:16287254-Tissue Distribution,
pubmed-meshheading:16287254-Transplantation, Heterologous
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| pubmed:articleTitle |
Evaluation of ((4-hydroxyphenyl)ethyl)maleimide for site-specific radiobromination of anti-HER2 affibody.
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| pubmed:affiliation |
Department of Chemistry, Organic Chemistry, Uppsala University, Uppsala, Sweden.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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