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单克隆抗体—苯丁酸氮芥靶向治癌偶联物的研究 被引量:1

Studies on the Targeted Monoclonal Antibody-Chlorambucil Conjugate for the Treatment of Cancer
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摘要 利用单克隆抗体对肿瘤细胞的特异选择性,制备了苯丁酸氮芥免疫毒素,首次发现苯丁酸氮芥的N—羟基琥珀酰亚胺酯的添加所用的时间对苯丁酸氮芥偶联的分子数和单克隆抗体的收率具有决定性的作用。本文研究了保持抗体与苯了酸氮芥的活性和提高单克隆抗体的收率、提高偶联的苯丁酸氮芥的分子数的最佳反应条件。通过体外细胞实验,证明该靶向药物具有明显的选择性杀伤癌细胞的功能。 The alkylating agent, chlorambucil (CBL), was attached to tumor-specific monoclonal antibody DX-86 with the CBL active ester method. The CBL active ester was obtained by the reaction between CBL and N-hydroxysuccinimide in the presence of N, N-dicyc-lohexylcarbodiimide. The number of CBL incorporated per molecular McAb was associated not only with the ratiq of CBL active ester to McAb, but also with the mixed time between the actiye .est&r and. McAb. The best reactive conditions were determined in this experiment. The result showed that this immunoconjugate has highly specific activity in the treatment of tumor cell in vitro and the activity of CBL and McAb was remained Therefore McAb-CBL conjugate could be therapeutically useful
出处 《免疫学杂志》 CAS CSCD 北大核心 1989年第2期17-20,共4页 Immunological Journal
关键词 单克隆抗体 苯丁酸氮芥 免疫毒素 Chlorambucil,Monoclonal antibody,Immunotoxin
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  • 1Kalaycio M. Bendamustine:a new look at an old drug[ J ]. Cancer,2009,27(25) :4 188-4 196.
  • 2Greig N H, Daly E M, Sweeney D J, et al. Harmacokinet- ics of chlorambucil-tertiary butyl ester, a lipophilic chlor, ambucil derivative that achieves and maintains high con- centrations in brain[ J]. Cancer Chemoth Pharm, 1990,25 (5) :320-325.
  • 3沈志祥.Prednimustine(泼尼氮芥)治疗乳腺癌的临床研究[J].中国肿瘤临床.1988,15(1):55-58.
  • 4Manolis A F, Anna I K, Evaggelia S A, et al. Structure-an-ti-leukemic activitychlorambucil relationship study of B- and D-ring modified and non-modified steroidal esters of chlorambucil [ J ]. Anti-Cancer Drugs, 2006, 17 ( 5 ) : 511- 519.
  • 5Gong Li,Qi Sun,Jing-Rong Cui,et al. Modification of the alkylating agent chlorambucil with spiropiperazinium salts [ J ], J Chin Pharma Sci,2010,19 (5) : 346-352.
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