Eötvös Loránd University, Research Group of Peptide Chemistry, Hungarian Academy of Sciences, 1117 Budapest, Hungary.
Expert Opin Drug Deliv. 2010 Jan;7(1):79-96. doi: 10.1517/17425240903418410.
Tumor targeting with peptides is based on the discovery that receptors for many regulatory peptides are overexpressed in tumor cells, compared with their expression in normal tissues. Consequently, these peptides and their analogues can be used as carriers/targeting moieties for the preparation of diagnostic and therapeutic agents that have increased selectivity and decreased peripheral toxicity.
Here an overview is given of the most relevant gonadotropin-releasing hormone (GnRH) and somatostatin derivatives, as well as of their applications in cancer diagnosis and therapy. For this purpose, recently published data in these areas (mostly articles published from 2000 to 2009) were reviewed.
In contrast to other regulatory peptides that stimulate the tumor growth, GnRH and somatostatin derivatives have inhibitory effect; therefore, they were used primarily for the preparation of various conjugates to be used in targeted chemotherapy, targeted radiotherapy, photodynamic therapy, boron neutron capture therapy and cancer diagnosis. Some of these conjugates have already found clinical applications, whereas others are now in preclinical and clinical trials.
Tumor targeting with hormone peptides provides a basis for the development of new diagnostic and therapeutic approaches for cancer.
肿瘤靶向肽是基于这样的发现，即许多调节肽的受体在肿瘤细胞中过度表达，与在正常组织中的表达相比。因此，这些肽及其类似物可用作载体/靶向部分，用于制备具有增加的选择性和降低的外周毒性的诊断和治疗剂。
本篇综述涵盖了最相关的促性腺激素释放激素（GnRH）和生长抑素衍生物，以及它们在癌症诊断和治疗中的应用。为此，审查了这些领域最近发表的数据（主要是 2000 年至 2009 年发表的文章）。
与其他刺激肿瘤生长的调节肽不同，GnRH 和生长抑素衍生物具有抑制作用；因此，它们主要用于制备各种用于靶向化疗、靶向放射治疗、光动力治疗、硼中子俘获治疗和癌症诊断的缀合物。其中一些缀合物已经找到了临床应用，而其他的则处于临床前和临床试验阶段。
激素肽的肿瘤靶向为癌症的新诊断和治疗方法的发展提供了基础。
