Metastasis is one of the major causes of death in patients with cancer, and cell invasion plays a fundamental part in this process. Because of the absence of efficacious treatments, caring for these patients is challenging. Recently, we optimized the structure of the naturally occurring lasso peptide sungsanpin. We identified two peptides, octapeptide and cyclic peptide which inhibited invasion into A549 cells effectively. We undertook an alanine scan of to explore the structure–activity relationship. The linear octapeptide and cyclic peptide exhibited improved inhibition of invasion into A549 cells. We modified to obtain , which displayed much higher inhibitory activity against invasion into A549 cells than . Of all peptides tested, upregulated significantly mRNA of tissue inhibitor matrix metalloproteinase TIMP-1 and TIMP-2.

中文翻译：

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宋三平衍生物作为细胞侵袭抑制剂的进一步结构优化和SAR研究

转移是癌症患者死亡的主要原因之一，细胞侵袭在这一过程中发挥着重要作用。由于缺乏有效的治疗方法，照顾这些患者具有挑战性。最近，我们优化了天然存在的套索肽sungsanpin的结构。我们鉴定出两种肽，八肽和环肽，可以有效抑制对A549细胞的侵袭。我们进行了丙氨酸扫描以探索结构-活性关系。线性八肽和环肽表现出改善的对 A549 细胞侵袭的抑制作用。我们对其进行了修饰，获得了比 .在所有测试的肽中，组织抑制剂基质金属蛋白酶 TIMP-1 和 TIMP-2 的 mRNA 显着上调。