Ríhová B, Kopecek J, Kopecková-Rejmanová P, Strohalm J, Plocová D, Semorádová H
J Chromatogr. 1986 Apr 11;376:221-33.
Soluble synthetic copolymers based on N-(2-hydroxypropyl)methacrylamide (HPMA) containing different oligopeptide side-sequences were tested as transport molecules for drugs and anti-Thy 1.2 antibodies in affinity therapy. As target cells, T lymphocytes were studied. (1) HPMA copolymers containing targeting anti-Thy 1.2 antibodies are 70 times more cytotoxic against T lymphocytes than HPMA copolymers with non-specific immunoglobulin. (2) Daunomycin conjugated to a biodegradable side-sequence (Gly-Phe-Leu-Gly) is effective in a concentration 100 times lower than daunomycin conjugated to a non-cleavable sequence (Gly-Gly). (3) HPMA copolymers containing drug and targeting antibodies are effective both in vitro and in vivo.
基于N-(2-羟丙基)甲基丙烯酰胺(HPMA)且含有不同寡肽侧序列的可溶性合成共聚物,作为药物和抗Thy 1.2抗体在亲和治疗中的转运分子进行了测试。以T淋巴细胞作为靶细胞进行研究。(1)含有靶向抗Thy 1.2抗体的HPMA共聚物对T淋巴细胞的细胞毒性比含有非特异性免疫球蛋白的HPMA共聚物高70倍。(2)与可生物降解侧序列(甘氨酸-苯丙氨酸-亮氨酸-甘氨酸)偶联的柔红霉素,其有效浓度比与不可裂解序列(甘氨酸-甘氨酸)偶联的柔红霉素低100倍。(3)含有药物和靶向抗体的HPMA共聚物在体外和体内均有效。