Hudecz F
Research Group for Peptide Chemistry, Hungarian Academy of Science, Eötvös L University, Budapest.
Anticancer Drugs. 1995 Apr;6(2):171-93. doi: 10.1097/00001813-199504000-00001.
New groups of synthetic biodegradable branched chain polypeptides have been prepared with the general formula poly[Lys-(Xi-DL-Alam)] or poly[Lys-(DL-Alam-Xi)] [AXK], where m approximately 3 and i < 1, and used to elucidate structural and functional properties required for the selection of macromolecular carriers for (i) targeting/delivery of antitumor agents (e.g. daunomycin, methotrexate, boron derivatives), peptide hormones (e.g. GnRH antagonist) or radionuclides for imaging (e.g. 123I, 111In, 51Cr) or therapy (e.g. 153Sm, 131I) or (ii) the construction of synthetic antigens with peptide epitopes of mucin or Herpes Simplex virus glycoprotein D. Principles applicable for a rational carrier design are outlined based on chemical (size, charge, solution conformation) and biological (cytotoxicity, pirogenicity, biodegradation, immunogenicity, immunomodulatory potential, biodistribution) characterization of these biopolymers and their conjugates.
已经制备了通式为聚[赖氨酸-(Xi-DL-丙氨酸)]或聚[赖氨酸-(DL-丙氨酸-Xi)] [AXK]的新型合成可生物降解支链多肽，其中m约为3且i < 1，并用于阐明选择大分子载体所需的结构和功能特性，这些载体用于：(i) 抗肿瘤剂（如柔红霉素、甲氨蝶呤、硼衍生物）、肽激素（如GnRH拮抗剂）或用于成像（如123I、111In、51Cr）或治疗（如153Sm、131I）的放射性核素的靶向/递送；或(ii) 构建具有粘蛋白或单纯疱疹病毒糖蛋白D肽表位的合成抗原。基于这些生物聚合物及其缀合物的化学（大小、电荷、溶液构象）和生物学（细胞毒性、致热原性、生物降解、免疫原性、免疫调节潜力、生物分布）表征，概述了适用于合理载体设计的原则。
