Introduction of five potentially metabolizable linking groups between 111In-cyclohexyl EDTA derivatives and F(ab')2 fragments of anti-carcinoembryonic antigen antibody--I. A new reproducible synthetic method.
The purpose of this study was to synthesize new bifunctional linker-chelating agents for the modification of the in vivo distribution of 111In-labeled antibodies. A general simple synthetic method of preparing cyclohexyl EDTA (CDTA) derivatives containing a linker/spacer group is described. Linkers prepared included a diester, a six carbon aliphatic chain, two thioethers and a disulfide group. The CDTA-linker compounds were coupled to F(Ab')2 fragments of anti-carcinoembryonic antigen monoclonal antibody and labeled with 111In with good retention of immunoreactivity.
Gestin
J F
JF
INSERM Unit 211, Nantes, France.
Faivre-Chauvet
A
A
Mease
R C
RC
Sai-Maurel
C
C
Thédrez
P
P
Slinkin
M
M
Meinken
G E
GE
Srivastava
S C
SC
Chatal
J F
JF
D000818:Animals; D002272:Carcinoembryonic Antigen / Q000276:immunology*; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D003432:Cross-Linking Reagents / Q000138:chemical synthesis* / Q000378:metabolism; D004355:Drug Stability; D004492:Edetic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D007128:Immunoglobulin Fragments / Q000737:chemistry* / Q000378:metabolism; D007205:Indium Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling / Q000379:methods; D051379:Mice; D015203:Reproducibility of Results
D002272:Carcinoembryonic Antigen; D002614:Chelating Agents; D003432:Cross-Linking Reagents; D007128:Immunoglobulin Fragments; D007205:Indium Radioisotopes; C005390:CDTA; D004492:Edetic Acid