The Institute for Quantitative Health Science & Engineering, Michigan State University, East Lansing, MI 48824, USA.
Comparative Medicine and Integrative Biology, College of Veterinary Medicine, Michigan State University, East Lansing, MI 48824, USA.
Int J Mol Sci. 2024 Aug 5;25(15):8553. doi: 10.3390/ijms25158553.
The burgeoning field of cancer theranostics has witnessed advancements through the development of targeted molecular agents, particularly peptides. These agents exploit the overexpression or mutations of specific receptors, such as the Epidermal Growth Factor receptor (EGFR) and αβ integrin, which are pivotal in tumor growth, angiogenesis, and metastasis. Despite the extensive research into and promising outcomes associated with antibody-based therapies, peptides offer a compelling alternative due to their smaller size, ease of modification, and rapid bioavailability, factors which potentially enhance tumor penetration and reduce systemic toxicity. However, the application of peptides in clinical settings has challenges. Their lower binding affinity and rapid clearance from the bloodstream compared to antibodies often limit their therapeutic efficacy and diagnostic accuracy. This overview sets the stage for a comprehensive review of the current research landscape as it relates to EGFR- and integrin αβ-targeting peptides. We aim to delve into their synthesis, radiolabeling techniques, and preclinical and clinical evaluations, highlighting their potential and limitations in cancer theranostics. This review not only synthesizes the extant literature to outline the advancements in peptide-based agents targeting EGFR and integrin αβ but also identifies critical gaps that could inform future research directions. By addressing these gaps, we contribute to the broader discourse on enhancing the diagnostic precision and therapeutic outcomes of cancer treatments.
癌症治疗诊断学领域的蓬勃发展见证了通过开发靶向分子药物，特别是肽，所取得的进步。这些药物利用特定受体的过度表达或突变，如表皮生长因子受体（EGFR）和αβ整合素，这些受体在肿瘤生长、血管生成和转移中起着关键作用。尽管针对基于抗体的治疗方法进行了广泛的研究并取得了有希望的结果，但由于其体积更小、修饰更容易和生物利用度更快，肽提供了一个引人注目的替代方案，这些因素可能会增强肿瘤穿透性并降低全身毒性。然而，肽在临床环境中的应用存在挑战。与抗体相比，它们的结合亲和力较低，从血液中清除速度较快，这通常会限制其治疗效果和诊断准确性。
本篇综述为全面回顾与 EGFR 和整合素 αβ 靶向肽相关的当前研究现状奠定了基础。我们旨在深入探讨它们的合成、放射性标记技术以及临床前和临床评估，强调它们在癌症治疗诊断学中的潜力和局限性。本综述不仅综合了现有文献，概述了针对 EGFR 和整合素 αβ 的基于肽的药物的进展，还确定了可能为未来研究方向提供信息的关键差距。通过解决这些差距，我们为提高癌症治疗的诊断精度和治疗效果的更广泛讨论做出了贡献。
