Guodong Li*, Shuyi Song, Baomei Yuan, Guangming Wan and Shenghua Zhang
School of Life Sciences, Zhengzhou University, ChinaFulltext PDF
Immunotherapy has become a major treatment in oncology. However, most cancer patients do not currently benefit from this treatment. In most patients with solid tumors, abnormal blood vessels help the tumor evade the attack of the immune system, with the blood vessel abnormalities being the result of elevated angiogenic factors such as Vascular Endothelial Growth Factor (VEGF) and angiopoietin 2. The use of drugs targeting these molecules normalizes the abnormal tumor vascular system to increase the infiltration of immune effect or cells and improve the responsiveness of immunotherapy. AS16 is a double-target peptide that is able to block both the VEGF and Tie2 signaling pathways, demonstrating significant anti-angiogenesis and antitumor effects. However, owing to its poor stability and short half-life, its clinical application is limited. To solve these problems, we used fixed-point modification of AS16 with Polyethylene Glycol (PEG) of different molecular weights to obtain PEG-AS16. The stability and half-life of the obtained PEG-AS16 were both longer than those of AS16. In addition, the biological activity of PEG-AS16 and its antiangiogenesis and anti tumor effects were demonstrated by wound healing assay of alginate-coated tumor cells. Our results suggest that PEG-AS16 has potential as an effective anti-angiogenesis drug.
Anti-angiogenesis; PEGylation; Anti-tumor; Peptide
Li G, Song S, Yuan B, Wan G, Zhang S. PEGylation of AS16 Double-Target Peptide that Blocks the Neuropilin-1 and Tie2 Signaling Pathways Enhances its Antitumor Effect. Clin Oncol. 2022;7:1893..