2F-Peracetyl-Fucose is a fucosyltransferase (FUT) inhibitor[1].
In vitro, 2F-Peracetyl-Fucose (0, 25, 50, 100 and 200μM; 24h or 1h) suppressed transforming growth factor β (TGFβ)-mediated Smad3 phosphorylation and nuclear translocation in NSCLC cells[1]. The U251-MG cells treated with 2F-Peracetyl-Fucose (200μM; 5 days) were more sensitive to temozolomide (TMZ) administration. Moreover, treatment with 2F-Peracetyl-Fucose (200μM; 24h) also inhibited the Transwell invasion of U251-MG cells[2]. 2F-Peracetyl-Fucose (300μM; 72h) had no effect on healthy NP cells and further reduced collagen type 2 (COL2) expression in inflamed Nucleus Pulposus Cells (NP cells)[3].
In vivo, After being treated with 20µg/ml of 2F-Peracetyl-Fucose for 96 hours, Calu-1-Luc cells exhibited reduced metastatic capacity in a mouse model of non-small cell lung cancer (NSCLC) metastasis[1]. 2F-Peracetyl-Fucose (500μM; 0, 1, 3, 5 and 7 days) inhibits head regeneration in Dugesia japonica after anterior pharynx amputation[4].
References:
[1] Park S, Lim JM, Chun JN, et al. Altered expression of fucosylation pathway genes is associated with poor prognosis and tumor metastasis in non‑small cell lung cancer. Int J Oncol. 2020 Feb;56(2):559-567.
[2] Wei KC, Lin YC, Chen CH, et al. Fucosyltransferase 8 modulates receptor tyrosine kinase activation and temozolomide resistance in glioblastoma cells. Am J Cancer Res. 2021 Nov 15;11(11):5472-5484.
[3] Joyce K, Mohd Isa IL, Krouwels A, et al. The role of altered glycosylation in human nucleus pulposus cells in inflammation and degeneration. Eur Cell Mater. 2021 Mar 28;41:401-420.
[4] Wang W, Yu Y, Liu H, et al. Protein Core Fucosylation Regulates Planarian Head Regeneration via Neoblast Proliferation. Front Cell Dev Biol. 2021 Jul 16;9:625823.
2F-Peracetyl-Fucose是岩藻糖基转移酶（FUT）抑制剂[1]。
在体外实验中，2F-Peracetyl-Fucose（0, 25, 50, 100和200μM; 24小时或1小时）抑制了非小细胞肺癌（NSCLC）细胞中转化生长因子β（TGFβ）介导的Smad3磷酸化及其核转位[1]。用2F-Peracetyl-Fucose（200μM; 5天）处理的U251-MG细胞对替莫唑胺（TMZ）治疗更为敏感。此外，2F-Peracetyl-Fucose（200μM; 24小时）的处理还抑制了U251-MG细胞的Transwell侵袭能力[2]。2F-Peracetyl-Fucose（300μM; 72h）对健康的髓核细胞（NP细胞）没有影响，但降低了炎症髓核细胞中Ⅱ型胶原（COL2）的表达[3]。
在体内实验中，Calu-1-Luc细胞经20µg/ml的2F-Peracetyl-Fucose处理96小时后，在小鼠非小细胞肺癌（NSCLC）转移模型中，Calu-1-Luc细胞转移能力受到抑制[1]。2F-Peracetyl-Fucose（500μM; 0, 1, 3, 5和7天）在截断了前端咽部的日本三角涡虫（Dugesia japonica）中抑制了头部再生[4]。