Schally Andrew V, Nagy Attila
Endocrine, Polypeptide, and Cancer Institute, Veterans Affairs Medical Center, New Orleans, LA 70112, USA.
Life Sci. 2003 Apr 11;72(21):2305-20. doi: 10.1016/s0024-3205(03)00113-9.
The development of targeted cytotoxic analogs of hypothalamic peptides for the therapy of various cancers is reviewed and various oncological studies on experimental tumors are summarized. Novel therapeutic modalities for breast, prostate and ovarian cancer consist of the use of targeted cytotoxic analogs of LH-RH containing doxorubicin (DOX) or 2-pyrrolino-DOX. The same radicals have been incorporated into cytotoxic analogs of somatostatin which can be also targeted to receptors for this peptide in prostatic, mammary, ovarian, renal and lung cancers, brain tumors and their metastases. A targeted cytotoxic analog of bombesin containing 2-pyrrolino-DOX has also been synthesized and successfully tried in experimental models of prostate cancer, small cell lung carcinoma and brain tumors. The development of these new classes of peptide analogs should lead to a more effective treatment for various cancers.
本文综述了用于治疗各种癌症的下丘脑肽靶向细胞毒性类似物的开发,并总结了对实验性肿瘤的各种肿瘤学研究。乳腺癌、前列腺癌和卵巢癌的新型治疗方法包括使用含有阿霉素(DOX)或2-吡咯啉-DOX的促黄体生成素释放激素(LH-RH)靶向细胞毒性类似物。相同的基团已被引入生长抑素的细胞毒性类似物中,其也可靶向前列腺癌、乳腺癌、卵巢癌、肾癌和肺癌、脑肿瘤及其转移灶中该肽的受体。一种含有2-吡咯啉-DOX的蛙皮素靶向细胞毒性类似物也已合成,并在前列腺癌、小细胞肺癌和脑肿瘤的实验模型中成功进行了试验。这些新型肽类似物的开发应能为各种癌症带来更有效的治疗。