PREPARATION OF HYDRAZINO-MODIFIED PROTEINS AND THEIR USE FOR THE SYNTHESIS OF TC-99M-PROTEIN CONJUGATES
PREPARATION OF HYDRAZINO-MODIFIED PROTEINS AND THEIR USE FOR THE SYNTHESIS OF TC-99M-PROTEIN CONJUGATES
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DOI：
10.1021/bc00011a007
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发表时间：
1991-09-01
影响因子：
4.7
通讯作者：
ZUBIETA, JA
中科院分区：
文献类型：
--
作者：
SCHWARTZ, DA;ABRAMS, MJ;ZUBIETA, JA
介绍了4-肼基苯甲酸琥珀酰亚胺盐酸盐(SHBH)和6-肼烟酸琥珀酰亚胺盐酸盐(SHNH)这两种新型双官能团连接剂的合成及其蛋白质连接性能。由于苯肼部分的存在，SHBH修饰的蛋白质是不稳定的。通过合成联氨基吡啶类似物SHNH，克服了这一问题，并得到了稳定的连接物。TC(V)氧代前体很容易添加到联氨吡啶修饰的蛋白质中，得到所需的~(99)TC-放射性标记蛋白质。~(99)M-联氨基吡啶-多克隆免疫球蛋白结合物是一种有用的感染灶显像剂。
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.