Enhanced kidney clearance with an ester-linked 99mTc-radiolabeled antibody Fab'-chelator conjugate

Journal Article · Wed Oct 31 23:00:00 EST 1990 · Bioconjugate Chemistry; (United States)

DOI:https://doi.org/10.1021/bc00006a010· OSTI ID:5317004

Weber, R W; Boutin, R H; Nedelman, M A; Lister-James, J; Dean, R T ^[1]

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1. Centocor, Inc., Malvern, PA (USA)

Bifunctional chelators for labeling antibodies with 99mTc based on the N3S core of (mercaptoacetyl)-triglycine having ester or amide linking moieties were synthesized and site-specifically attached to the sulfhydryl groups of the Fab' fragment of antimyosin. Protein labeling was quantitative after 15 min; postlabeling purification was not necessary. The radiolabeled conjugates exhibited no loss of immunoreactivity. Under basic conditions, the ester-linked conjugate lost 95% of the radiolabel in the form of the 99mTc complex of (mercaptoacetyl)triglycine as determined by RP-HPLC, while the radioactivity in the amide-linked conjugate remained completely bound to the protein. In a mouse biodistribution study, the ester-linked conjugate showed a 2-fold enhancement in clearance from the kidney when compared to the amide-linked product.

• OSTI ID: 5317004
• Journal Information: Bioconjugate Chemistry; (United States), Journal Name: Bioconjugate Chemistry; (United States) Vol. 1:6; ISSN 1043-1802; ISSN BCCHE
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AMIDES
ANIMALS
ANTIBODIES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CHROMATOGRAPHY
CLEARANCE
DISTRIBUTION
ESTERS
EXCRETION
GLOBULINS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
INTERNAL CONVERSION RADIOISOTOPES
ISOMERIC NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KIDNEYS
LABELLING
LIQUID COLUMN CHROMATOGRAPHY
MAMMALS
MICE
MOLECULAR STRUCTURE
MYOSIN
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
RADIOISOTOPES
RENAL CLEARANCE
RODENTS
SEPARATION PROCESSES
STRUCTURE-ACTIVITY RELATIONSHIPS
TECHNETIUM 99
TECHNETIUM ISOTOPES
TISSUE DISTRIBUTION
TRACER TECHNIQUES
VERTEBRATES
YEARS LIVING RADIOI