2024年2月1日 · N-terminal processing by methionine aminopeptidases (MetAP) is a crucial step in the maturation of proteins during protein biosynthesis. Small-molecule inhibitors of MetAP2 have antiangiogenic and antitumoral activity. Herein, we characterize the structurally novel MetAP2 inhibitor M8891. M8891 is a …

2024年2月1日 · N-terminal processing by methionine aminopeptidases (MetAP) is a crucial step in the maturation of proteins during protein biosynthesis. Small-molecule inhibitors of MetAP2 have antiangiogenic and antitumoral activity. Herein, we characterize the structurally novel MetAP2 inhibitor M8891.

2017年11月8日 · MetAP2 knockdown decreased vascular endothelial growth factor (VEGF) secretion and expression at the mRNA and protein levels. Decreased VEGF expression in MetAP2 knockdown cells correlated very well with decreased vessel …

新鉴定的 MetAP2 底物翻译延伸因子 1-α-1 (EF1a-1) 可作为药效生物标志物，用于跟踪细胞和小鼠研究中的靶点抑制。 M8891 单一疗法观察到强大的血管生成和肿瘤生长抑制作用。

2009年5月1日 · Decrease in VEGF correlated very well with tube formation assay as demonstrated by decreased vessel formation by MetAP-2 knockdown cells. To further study the mechanism underlying MetAP2 down regulating VEGF, we used dual-luciferase reporter driving different length of VEGF promoters and performed a luciferase assay.

MetAP2 knockdown decreased vascular endothelial growth factor (VEGF) secretion and expression at the mRNA and protein levels. Decreased VEGF expression in MetAP2 knockdown cells correlated very well with decreased vessel formation in a tube formation assay.

MetAP2 knockdown resulted in disruption of capillary-like structures in vitro. Experiment was repeated thrice and micrographs of typical fields illustrate HUVEC tube formation under various...

2014年5月20日 · Background: Fumagillol derivatives are novel anti-angiogenic agents that inhibit methionine aminopeptidase 2 (MetAP2) rather than directly inhibiting VEGF signaling. Clinical development of fumagillol derivatives (e.g. TNP-470) has been limited by …

ABSTRACT N-terminal processing by methionine aminopeptidases (MetAP) is a crucial step in the maturation of proteins during protein biosynthesis. Small-molecule inhibitors of MetAP2 have antiangiogenic and antitumoral activity. Herein, we characterize the structurally novel MetAP2 inhibitor M8891.

This report describes the physicochemical and pharmacological characterization of SDX-7320 (evexomostat), a polymer–drug conjugate of the novel METAP2 inhibitor (METAP2i) SDX-7539. In vitro binding, enzyme, and cell-based assays demonstrated that SDX-7539 is a potent and selective METAP2 inhibitor.