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Misonidazole was covalently conjugated (3-68 mol drug/mol antibody) to 19-9 monoclonal antibody directed against a colorectal carcinoma tumor-associated antigen as a method for targeting radiosensitizing agents. This attachment was accomplished by the mixed anhydride method using the hemisuccinate derivative of misonidazole. Evaluation of conjugates in vitro shows a loss of antibody binding activity with increasing loading levels; however, significant binding activity is retained even at relatively high sensitizer/antibody ratios. This observation was consistent in three binding assays: a competitive radioimmunoassay; an enzyme immunoassay; and an affinity column assay. From these studies, it was concluded that the optimal loading factor for misonidazole-antibody conjugates, when it is used for immunochemotherapy lies between 8 and 15. In vitro release studies indicated that conjugates are hydrolytically stable (t1/2 = 4 days) under physiological conditions.
K P Borlinghaus, and
D A Fitzpatrick, and
N D Heindel, and
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B A Mease, and
K J Schray, and
D J Shealy, and
H L Walton, and
D V Woo
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K P Borlinghaus, and
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H L Walton, and
D V Woo
January 1983,
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K P Borlinghaus, and
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K P Borlinghaus, and
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D V Woo
May 1985,
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K P Borlinghaus, and
D A Fitzpatrick, and
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K J Schray, and
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H L Walton, and
D V Woo
February 1986,
Archives of biochemistry and biophysics,
K P Borlinghaus, and
D A Fitzpatrick, and
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H L Walton, and
D V Woo
October 2013,
Bioconjugate chemistry,
K P Borlinghaus, and
D A Fitzpatrick, and
N D Heindel, and
J A Mattis, and
B A Mease, and
K J Schray, and
D J Shealy, and
H L Walton, and
D V Woo
January 1986,
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K P Borlinghaus, and
D A Fitzpatrick, and
N D Heindel, and
J A Mattis, and
B A Mease, and
K J Schray, and
D J Shealy, and
H L Walton, and
D V Woo
January 1983,
Cancer immunology, immunotherapy : CII,
K P Borlinghaus, and
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J A Mattis, and
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K J Schray, and
D J Shealy, and
H L Walton, and
D V Woo
March 1983,
Clinical chemistry,
K P Borlinghaus, and
D A Fitzpatrick, and
N D Heindel, and
J A Mattis, and
B A Mease, and
K J Schray, and
D J Shealy, and
H L Walton, and
D V Woo
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International journal of cancer,
