Engel Jörg B, Schally Andrew V, Dietl Johannes, Rieger Lorenz, Hönig Arnd
Universitätsfrauenklinik Würzburg, Josef-Schneider-Strasse 4, 97080 Würzburg, Germany.
Mol Pharm. 2007 Sep-Oct;4(5):652-8. doi: 10.1021/mp0700514. Epub 2007 Aug 18.
Gynecological cancers such as breast, ovarian, and endometrial carcinoma express receptors for luteinizing hormone-releasing hormone (LHRH), bombesin/gastrin-releasing peptide (BN/GRP), and somatostatin (SST). These tumors are therefore suitable candidates for targeted therapy with cytotoxic hybrid molecules consisting of a cytotoxic radical and a peptide hormone analogue as a carrier. These compounds have been shown to be more active and less toxic in vivo than nontargeted chemotherapy in models of various human cancers which express the respective receptors. The current review summarizes experimental and clinical findings with cytotoxic peptide hormone analogues of LHRH (AN-152 [AEZS 108], AN-207), BN/GRP (AN-215), and SST (AN-238) in breast, ovarian, and endometrial cancers.
妇科癌症，如乳腺癌、卵巢癌和子宫内膜癌，表达促黄体生成激素释放激素（LHRH）、蛙皮素/胃泌素释放肽（BN/GRP）和生长抑素（SST）的受体。因此，这些肿瘤适合用由细胞毒性基团和作为载体的肽激素类似物组成的细胞毒性杂交分子进行靶向治疗。在各种表达相应受体的人类癌症模型中，这些化合物在体内已显示出比非靶向化疗更具活性且毒性更小。本综述总结了LHRH（AN - 152 [AEZS 108]、AN - 207）、BN/GRP（AN - 215）和SST（AN - 238）的细胞毒性肽激素类似物在乳腺癌、卵巢癌和子宫内膜癌中的实验和临床研究结果。
