Affibody (affibody) ligands that are specific for the extracellular domain of human epidermal growth factor receptor 2 (HER2/neu) have been selected by phage display technology from a combinatorial protein library based on the 58 amino acid residue staphy
Kahalalide F 是一种海洋来源的抗肿瘤剂,能够抑制DNA合成(DNA synthesis)。其细胞毒性与多药耐药基因MDR1和酪氨酸激酶HER2/NEU的表达无关,仅与抗凋亡蛋白BCL-2的表达略有相关。Kahalalide F 通过耗竭ErbB3抑制PI3K-Akt信号通路,并且短时脉冲处理即可激活其作用,主要通过肿瘤细胞胀亡(oncosis)诱导细胞死亡。Kahalalide F 可用于研究前列腺癌、乳腺癌、外阴癌和非小细胞肺癌。
Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.