Schally Andrew V, Block Norman L, Rick Ferenc G
Veterans Affairs Medical Center and South Florida Veterans Affairs Foundation for Research and Education, Miami, Florida.
Department of Pathology, University of Miami Miller School of Medicine, Miami, Florida.
Prostate. 2017 Jun;77(9):1036-1054. doi: 10.1002/pros.23360. Epub 2017 Apr 27.
The discovery, isolation, elucidation of structure, synthesis, and initial testing of the neuropeptide hypothalamic luteinizing hormone-releasing hormone (LHRH), which regulates reproduction, is briefly described. The design, synthesis, and experimental and clinical testing of agonistic analogs of LHRH is extensively reviewed focusing on the development of new methods for the treatment of prostate cancer. Subsequent development of antagonistic analogs of LHRH is then faithfully recounted with special emphasis on therapy of prostate cancer and BPH. The concepts of targeted therapy to peptide receptors on tumors are re-examined and the development of the cytotoxic analogs of LHRH and their status is reviewed. The endeavor to develop better therapies for prostate cancer, based on LHRH analogs, guided much of our work.
简要描述了调节生殖的神经肽下丘脑促黄体激素释放激素（LHRH）的发现、分离、结构阐明、合成及初步测试。重点围绕前列腺癌治疗新方法的开发，广泛综述了LHRH激动剂类似物的设计、合成以及实验和临床测试。接着如实叙述了LHRH拮抗剂类似物的后续开发情况，特别强调了其在前列腺癌和良性前列腺增生治疗方面的应用。重新审视了针对肿瘤上肽受体的靶向治疗概念，并综述了LHRH细胞毒性类似物的开发及其现状。基于LHRH类似物开发更好的前列腺癌治疗方法的努力，指导了我们的大部分工作。
