TY - JOUR
T1 - Improved synthesis of 6-[p-(bromoacetamido)benzyl]-1,4,8,11-tetraazacyclotetradecane-N,N′, N″,N‴-tetraacetic acid and development of a thin-layer assay for thiol-reactive bifunctional chelating agents
AU - Moran, Justin K.
AU - Greiner, Douglas P.
AU - Meares, Claude F.
PY - 1995
Y1 - 1995
N2 - Monoclonal antibodies labeled with radiometals such as copper-67 have applications in radioimmunodiagnosis and radioimmunotherapy. Moi et al. [(1985) Anal. Biochem. 148, 249-253] showed that 6-[p-(bromoacetamido)benzyl]-1,4,8,11-tetraazacyclotetradecane-N,N′, N″,N‴-tetraacetic acid (BAT) is an effective reagent for linking copper to proteins, and antibodies labeled with copper radionuclides are currently undergoing clinical trials. Here we describe improvements in the original synthesis that increase the overall yield of BAT to 23%. We also describe a new assay useful to determine the activity of bifunctional chelating agents with thiol-reactive functional groups.
AB - Monoclonal antibodies labeled with radiometals such as copper-67 have applications in radioimmunodiagnosis and radioimmunotherapy. Moi et al. [(1985) Anal. Biochem. 148, 249-253] showed that 6-[p-(bromoacetamido)benzyl]-1,4,8,11-tetraazacyclotetradecane-N,N′, N″,N‴-tetraacetic acid (BAT) is an effective reagent for linking copper to proteins, and antibodies labeled with copper radionuclides are currently undergoing clinical trials. Here we describe improvements in the original synthesis that increase the overall yield of BAT to 23%. We also describe a new assay useful to determine the activity of bifunctional chelating agents with thiol-reactive functional groups.
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M3 - Article
C2 - 7632802
AN - SCOPUS:0029300636
VL - 6
SP - 296
EP - 301
JO - Bioconjugate Chemistry
JF - Bioconjugate Chemistry
SN - 1043-1802
IS - 3
ER -