Radiolabeled peptide conjugates for targeting of the bombesin receptor superfamily subtypes
Radiolabeled peptide conjugates for targeting of the bombesin receptor superfamily subtypes
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DOI：
10.1016/j.nucmedbio.2005.05.005
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发表时间：
2005-10-01
影响因子：
3.1
通讯作者：
Hoffman, TJ
中科院分区：
文献类型：
--
作者：
Smith, CJ;Volkert, WA;Hoffman, TJ
世界各地的研究实验室目前正集中精力开发基于小肽如奥曲肽、神经降压素、α-黑素细胞刺激激素、血管肠肽等的放射性、定点诊断/治疗剂。蛙皮素（BBN）或蛙皮素的衍生物也具有重要意义。蛙皮素是一种对BB 2或胃泌素释放肽受体（GRPr）具有非常高亲和力的14个氨基酸的肽。GRPr在多种人类癌症上的过表达（即，乳腺、前列腺、胰腺、小细胞肺等）为开发用于靶向并因此诊断/治疗这些特定疾病的放射性BBN衍生物提供了潜在功效。正在开发新的衍生物，其也能够靶向在癌细胞上过表达的13131和13133受体亚型。这篇综述强调了在过去的2年中，BBN受体特异性放射性药物设计的一些最新进展。(c)2005年爱思唯尔公司All rights reserved.
Research laboratories around the world are currently focusing their efforts toward the development of radiometallated, site-directed, diagnostic/therapeutic agents based upon small peptides such as octreotide, neurotensin, alpha-melanocyte stimulating hormone, vasointestinal peptide and others. Bombesin (BBN) or derivatives of bombesin are also of significant interest. Bombesin is a 14-amino-acid peptide with very high affinity for the BB2 or gastrin-releasing peptide receptor (GRPr). Over-expression of the GRPr on a variety of human cancers (i.e., breast, prostate, pancreatic, small cell lung, etc.) provides potential efficacy toward development of radiometallated BBN derivatives for targeting and, hence, diagnosis/treatment of these specific diseases. New derivatives are being developed that are also capable of targeting the 1313 1 and 13133 receptor subtypes that are over-expressed on cancer cells. This review highlights some of the more recent developments toward design of BBN receptor-specific radiopharmaceuticals that have taken place over the past 2 years. (c) 2005 Elsevier Inc. All rights reserved.