摘要
背景:前列腺癌是世界上最常见的癌症之一,每年约有110万例确诊病例。分子成像的快速发展促进了对结构的进一步理解,这有助于制定治疗方案和更准确诊断的新组合,避免不必要的前列腺活检。这些累积的知识也对疾病的侵袭性阶段和肿瘤复发的提供了更好理解。最近,在开发拟肽基抑制剂作为有效结合前列腺特异性膜抗原(PSMA)——由前列腺癌细胞表达的——有前景的候选物方面取得了很大进展。目的:本文将广泛综述小分子和肽基PSMA抑制剂的最新进展,为未来PSMA抑制剂的合理设计提供基础。方法:本文回顾了1996年至2020年间研究的有关PSMA抑制剂的文献,强调了最近的合成进展和化学策略,同时强调了每种抑制剂的治疗潜力和缺点。结果:本综述中出现的PSMA合成抑制剂皆阐释了其在体内外的临床应用。结论:这篇综述强调了PSMA抑制剂的临床潜力,分析了所使用的化学合成方法的优点和缺点,为发现新的PSMA抑制剂用于未来的临床应用奠定了基础。
关键词: 前列腺特异性膜抗原抑制剂,肿瘤靶向性,正电子发射断层扫描(PET)成像,前列腺癌症。
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