LyP-1 TFA is a cyclic nonapeptide with tumor-targeting capability[1-2]. LyP-1 TFA can be used in research related to tumor-targeted therapy and molecular imaging[3-4].
In vitro, MDA-MB-435 human breast carcinoma cells were incubated with LyP-1 TFA (5-500µM) for 24-72 hours. LyP-1 TFA induced cell lysis and death in MDA-MB-435 cells in a dose-dependent manner. C8161 human melanoma cells were not affected by the peptide[5].
In vivo, nude mice bearing MDA-MB-435 or MDA-MB-435/VEGF-C tumors were treated with LyP-1 TFA (60µg; intravenous injection) twice a week for 4-5 weeks starting from when the tumors were palpable. LyP-1 TFA significantly inhibited tumor growth, while also inducing tumor cell apoptosis and reducing intratumoral lymphatic vessel density[5]. ApoE knockout mice were treated with LyP-1 TFA (200µg/day; intravenous injection) for 2-8 weeks. LyP-1 TFA significantly reduced the atherosclerotic plaque area induced by a high-fat diet and arterial ligation, exerting its anti-atherosclerotic effect by increasing apoptosis of macrophages within the plaques[6].
References:
[1] Zhang F, Niu G, Lin X, et al. Imaging tumor-induced sentinel lymph node lymphangiogenesis with LyP-1 peptide. Amino Acids. 2012 Jun;42(6):2343-51.
[2] Song N, Zhao L, Zhu M, et al. Recent progress in LyP-1-based strategies for targeted imaging and therapy. Drug Deliv. 2019 Dec;26(1):363-375.
[3] Lin QJ, Xie ZB, Gao Y, et al. LyP-1-fMWNTs enhanced targeted delivery of MBD1siRNA to pancreatic cancer cells. J Cell Mol Med. 2020 Mar;24(5):2891-2900.
[4] Song N, Zhao L, Xu X, et al. LyP-1-Modified Multifunctional Dendrimers for Targeted Antitumor and Antimetastasis Therapy. ACS Appl Mater Interfaces. 2020 Mar 18;12(11):12395-12406.
[5] Laakkonen P, Akerman ME, Biliran H, et al. Antitumor activity of a homing peptide that targets tumor lymphatics and tumor cells. Proc Natl Acad Sci U S A. 2004 Jun 22;101(25):9381-6.
[6] She ZG, Hamzah J, Kotamraju VR, et al. Plaque-penetrating peptide inhibits development of hypoxic atherosclerotic plaque. J Control Release. 2016 Sep 28;238:212-220.
LyP-1 TFA是一种具有肿瘤靶向能力的环状九肽[1-2]。LyP-1 TFA可用于肿瘤靶向治疗和分子成像的相关研究[3-4]。
在体外，LyP-1 TFA（5-500μM）孵育MDA-MB-435人乳腺癌癌细胞24-72小时。LyP-1 TFA以剂量依赖方式诱导MDA-MB-435发生细胞裂解与死亡。而C8161人黑色素瘤细胞则不受该肽的影响[5]。
在体内，LyP-1 TFA（60μg；静脉注射）经静脉注射处理携带MDA-MB-435或MDA-MB-435/VEGF-C肿瘤的裸鼠，每周两次，从肿瘤可触及后开始持续4-5周。LyP-1 TFA显著抑制了肿瘤生长，同时诱导了肿瘤细胞凋亡并减少了肿瘤内淋巴管数量[5]。LyP-1 TFA（200μg/天）经静脉注射处理ApoE基因敲除小鼠2-8周。LyP-1 TFA可显著减少由高脂饮食及动脉结扎诱导的动脉粥样硬化斑块面积，同时通过增加斑块内巨噬细胞的凋亡来发挥其抗动脉粥样硬化作用[6]。