POLYETHYLENE-GLYCOL MODIFICATION OF THE MONOCLONAL-ANTIBODY A7 ENHANCES ITS TUMOR-LOCALIZATION
POLYETHYLENE-GLYCOL MODIFICATION OF THE MONOCLONAL-ANTIBODY A7 ENHANCES ITS TUMOR-LOCALIZATION
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DOI：
10.1016/0006-291x(90)90839-f
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发表时间：
1990-09-28
影响因子：
3.1
通讯作者：
HAKOMORI, S
中科院分区：
文献类型：
--
作者：
KITAMURA, K;TAKAHASHI, T;HAKOMORI, S
小鼠单克隆抗体A7的F（ab”）2片段与聚乙二醇（PEG，分子量：5000）共价结合，并通过体外和体内研究将其与亲本F（ab”）2片段进行了比较。peg偶联抗体片段在竞争性放射免疫分析中保持其抗原结合活性。偶联物的半衰期较长，在肿瘤中的积累增加。虽然亲本F(ab ")2片段的肿瘤与血液比值高于偶联物，但其值高于整个单抗A7。与亲本F（ab”）2片段相比，偶联物对正常器官的吸收程度较低，组织与血液的比例较低。我们的研究结果表明，这种peg偶联的F(ab ")2片段可能是一种有希望用于靶向癌症化疗的载体。
The F(ab'')2 fragment of murine monoclonal antibody A7 was covalently bonded to polyethylene glycol (PEG, molecular weight: 5000) and the conjugate was compared to the parent F (ab'')2 fragment by in vitro and in vivo studies. PEG-conjugated antibody fragment retained its antigen-binding activity in a competitive radioimmunoassay. The conjugate had a longer half-life and showed increased accumulation in tumors. Although the tumor:blood ratio for parent F(ab'')2 fragment was higher than that for the conjugate, it showed higher value than whole MAb A7. The tissue:blood ratios were kept low with the conjugate, indicating that the conjugate was uptaken to normal organ with lesser extent, as compared with parent F(ab'')2 fragment. Our findings indicate that this PEG-conjugated F(ab'')2 fragment could be a promising carrier for use in targeting cancer chemotherapy.