Linked Life Data

8889020

Source:http://linkedlifedata.com/resource/pubmed/id/8889020

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
1997-2-4
pubmed:abstractText
Immunoconjugates sometimes suffer changes in immunoreactivity and tumor targeting because the chelators used interfere with antigen binding. To try to circumvent such problems, two new homobifunctional chelating agents, 2,6-bis[p-[(beta-maleimidopropionyl) amino]benzyl]diethylenetriamine- N,N,N',N",N"-pentaacetic acid (MPBz-DTPA) and 2,9-bis [p-(beta-maleimidopropionyl)amino]benzyl] triethylenetetraamine-N,N,N',N',N",N"-hexaacetic acid (MPBz-TTHA), were synthesized for chelation of 111In and 90Y metal ions. Each of the new chelators contains two maleimido functional groups substituted at the carbon backbone. In this study, the overall chemical yields for MPBz-DTPA and MPBz-TTHA were approximately 5 and 4%, respectively. The intermediate and final compounds were purified by flash chromatography and fully characterized by 1H-NMR, 13C-NMR, and mass spectroscopy. Chemical modification of the maleimido group on each of these derivatives allowed specific conjugation with a sulfhydryl group at the hinge region of an antibody molecule and conjugation with other peptides. For instance, the two Fab' fragments, through their hinge-region sulfhydryl groups, could covalently attach to a homobifunctional chelator via thioether linkage to generate a Fab'-S-chelator-S-Fab' immunoconjugate. By design, immunoconjugates containing these new chelators will contain only one chelator derivative at a known region of antibody away from the antigen binding site. Consequently, these chelators may minimize changes in the immunoreactivity and improve tumor targeting of immunoconjugates that contain them.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1043-1802
pubmed:author
pubmed:issnType
Print
pubmed:volume
7
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
576-83
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed:articleTitle
Maleimido derivatives of diethylenetriaminepentaacetic acid and triethylenetetraaminehexaacetic acid: their synthesis and potential for specific conjugation with biomolecules.
pubmed:affiliation
Department of Experimental Radiotherapy, University of Texas M.D. Anderson Cancer Center, Houston 77030, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.