PREPARATION OF HYDRAZINO-MODIFIED PROTEINS AND THEIR USE FOR THE SYNTHESIS OF TC-99M-PROTEIN CONJUGATES

被引:100
作者
SCHWARTZ, DA
ABRAMS, MJ
HAUSER, MM
GAUL, FE
LARSEN, SK
RAUH, D
ZUBIETA, JA
机构
[1] MCNEIL PHARMACEUT RES,SPRING HOUSE,PA 19477
[2] SYRACUSE UNIV,DEPT CHEM,SYRACUSE,NY 13244
关键词
D O I
10.1021/bc00011a007
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The syntheses and protein linking properties of succinimidyl 4-hydrazinobenzoate hydrochloride (SHBH) and succinimidyl 6-hydrazinonicotinate hydrochloride (SHNH), two new heterobifunctional linkers which lead to hydrazino-modified proteins, are described. SHBH-modified proteins are unstable due to the presence of the phenylhydrazine moiety. This problem was overcome by synthesizing the hydrazinopyridine analogue SHNH, and the conjugates derived from this linker are stable. Tc(V) oxo precursors readily add to hydrazinopyridine-modified proteins to yield the desired Tc-99m-radiolabeled protein. Tc-99m-hydrazinopyridine-polyclonal IgG conjugates are useful agents for the imaging of focal sites of infection.
引用
收藏
页码:333 / 336
页数:4
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