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Luteinizing hormone-releasing hormone receptor targeted agents for prostate cancer.

机译:黄体激素释放激素受体靶向药物,用于前列腺癌。

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INTRODUCTION: Receptors for luteinizing hormone-releasing hormone (LHRH) are expressed on a variety of human cancer cells with relatively limited expression in normal tissues. The selective and persistent expression of these receptors in prostate cancer cells is the rationale for LHRH receptor targeted agents. With many agents in development and one entering early clinical study, it is important to be familiar with the concept of LHRH receptor targeting and the evidence supporting its use. AREAS COVERED: This manuscript reviews the expression of LHRH receptors and the rationale for LHRH receptor targeted therapy in prostate cancer. Several different classes of agents targeting the LHRH receptor are discussed. The preclinical evidence supporting these agents is also reviewed and the clinical trial testing one of these agents is detailed. EXPERT OPINION: LHRH receptor expression on prostate cancer cells has led to the rational design of many new compounds. The preclinical evidence is encouraging for these agents, which are in varying phases of development. AN-152 combines a modified LHRH agonist carrier with doxorubicin and is entering a Phase I-II clinical study.
机译:简介:促黄体生成激素释放激素(LHRH)的受体在多种人类癌细胞中表达,在正常组织中的表达相对有限。这些受体在前列腺癌细胞中的选择性和持续表达是LHRH受体靶向药物的基本原理。随着许多药物的开发和一种药物进入早期临床研究,熟悉LHRH受体靶向的概念和支持其使用的证据非常重要。覆盖的区域:本手稿回顾了LHRH受体的表达以及LHRH受体靶向治疗前列腺癌的原理。讨论了针对LHRH受体的几种不同类别的药物。还审查了支持这些药物的临床前证据,并详细介绍了对其中一种药物的临床试验测试。专家意见:LHRH受体在前列腺癌细胞上的表达已导致许多新化合物的合理设计。这些药物处于发展的不同阶段,临床前证据令人鼓舞。 AN-152结合了改良的LHRH激动剂载体和阿霉素,目前正在进入I-II期临床研究。

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