Melton R G, Searle F, Sherwood R F, Bagshawe K D, Boden J A
Division of Biotechnology, PHLS Centre for Applied Microbiology and Research, Salisbury, Wilts, UK.
Br J Cancer. 1990 Mar;61(3):420-4. doi: 10.1038/bjc.1990.92.
The in vivo localising and clearance properties of conjugates of the folate-degrading enzyme carboxypeptidase G2 (CPG2) with anti-human chorionic gonadotrophin (W14A) were measured in nude mice bearing CC3 choriocarcinoma xenografts. Conjugates of W14A-F (ab')2 fragment coupled to CPG2 localised in tumour as effectively as native antibody alone but showed lower uptake in other major tissues. The clearance rates of conjugates prepared with intact antibody or F (ab')2 fragment were shown to be up to five-fold faster than for native antibody and two-fold compared to F (ab')2 fragment. Molecular weight analysis of residual conjugate in the blood showed that no degradation of conjugate to its component molecules occurred during circulation. It was concluded that F (ab')2: CPG2 conjugates offered the greatest potential for targeting applications.
在携带CC3绒毛膜癌异种移植瘤的裸鼠中，测定了叶酸降解酶羧肽酶G2（CPG2）与抗人绒毛膜促性腺激素（W14A）缀合物的体内定位和清除特性。与CPG2偶联的W14A - F（ab'）2片段缀合物在肿瘤中的定位效果与单独的天然抗体一样有效，但在其他主要组织中的摄取较低。完整抗体或F（ab'）2片段制备的缀合物的清除率比天然抗体快达五倍，与F（ab'）2片段相比快两倍。血液中残留缀合物的分子量分析表明，缀合物在循环过程中未降解为其组成分子。得出的结论是，F（ab'）2：CPG2缀合物在靶向应用方面具有最大潜力。
