Linked Life Data

10101833

Source:http://linkedlifedata.com/resource/pubmed/id/10101833

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1999-4-29
pubmed:abstractText
This laboratory uses an N-hydroxysuccinimide derivative of S-acetylmercaptoacetyltriglycine (NHS-MAG3) to conjugate amines for subsequent labeling with 99mTc. However, the synthesis from triglycerine is general and not restricted to this tripeptide. We had earlier selected a small number of alternative tripeptides and synthesized the corresponding NHS derivatives. Each was then evaluated in a search for bifunctional chelators with properties superior to NHS-MAG3, such as lower serum protein binding or improved stability to cysteine challenge. Based on these preliminary results, NHS-S-acetylmercaptoacetyltriserine (NHS-MAS3) was selected for further investigation. We have now conjugated this bifunctional chelator to an biocytin and to an amine-derivatized peptide nucleic acid (PNA). Both carriers were also conjugated with NHS-MAG3 under identical conditions and all were labeled with 99mTc at neutral pH and at boiling temperature while the conjugated PNAs were radiolabelled at neutral pH and at room temperature. Regardless of the chelator, reverse phase HPLC radiochromatograms of the labeled biotins and PNAs after purification showed a single peak. However, by size exclusion HPLC, the radiochromatograms always showed several peaks even after purification, but the MAS3 radiochromatograms were less complicated. For biotin and PNA both, radiolabeling via MAS3 showed improved 99mTc stability in 37 degrees C serum and in cysteine solution. The four preparations were administered to mice implanted in one thigh with avidin beads (biotins) or complementary PNA beads (PNAs). At 5 h post-administration, no significant differences were observed in the targeting of PNA beads between the two chelators, however the target thigh/normal thigh ratio was significantly higher for MAS3-biotin compared to MAG3-biotin. We conclude that labeling biocytin and amine-derivatized PNA with NHS-MAS3 compared to NHS-MAG3 provides simpler radiochromatographic profiles, improved stability of the label in serum and cysteine solution and can improve in vivo targeting.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0969-8043
pubmed:author
pubmed:issnType
Print
pubmed:volume
50
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
723-32
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed-meshheading:10101833-Animals, pubmed-meshheading:10101833-Biotin, pubmed-meshheading:10101833-Blood Proteins, pubmed-meshheading:10101833-Chelating Agents, pubmed-meshheading:10101833-Chromatography, Gel, pubmed-meshheading:10101833-Chromatography, High Pressure Liquid, pubmed-meshheading:10101833-Female, pubmed-meshheading:10101833-Glycine, pubmed-meshheading:10101833-Humans, pubmed-meshheading:10101833-Isotope Labeling, pubmed-meshheading:10101833-Male, pubmed-meshheading:10101833-Mice, pubmed-meshheading:10101833-Oligopeptides, pubmed-meshheading:10101833-Organotechnetium Compounds, pubmed-meshheading:10101833-Peptide Nucleic Acids, pubmed-meshheading:10101833-Protein Binding, pubmed-meshheading:10101833-Radiopharmaceuticals, pubmed-meshheading:10101833-Succinimides, pubmed-meshheading:10101833-Tissue Distribution
pubmed:year
1999
pubmed:articleTitle
NHS-MAS3: a bifunctional chelator alternative to NHS-MAG3.
pubmed:affiliation
Department of Nuclear Medicine, University of Massachusetts Medical Center, Worcester 01655, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.