Fz7-21 TFA ((Ac)-LPSDDLEFWCHVMY-NH2 TFA) 是 Frizzled 7 (FZD 7) 受体的肽拮抗剂,选择性地与 FZD7 CRD 亚类结合。在人和小鼠 FZD7 CRD 中的 EC50 值分别为 58 和 34 nM。Fz7-21 对外源性 WNT3A (IC50=100 nM) 刺激和转染 WNT3A 或 WNT1 的 HEK293 细胞 Wnt/β-catenin 信号传导有损伤。Fz7-21 还阻断了 WNT3A 介导的 β-catenin 在小鼠 L 细胞中
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Fz7-21 TFA ((Ac)-LPSDDLEFWCHVMY-NH2 TFA), a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM)[1].
[1]. Nile AH, et al. Publisher Correction: A selective peptide inhibitor of Frizzled 7 receptors disrupts intestinal stem cells. Nat Chem Biol. 2018 Sep;14(9):902.
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