Borrelidin
Angiogenesis inhibitor / Novel macrolide which inhibits bacterial and eukaryotic threonyl-tRNA synthetase.1 Displays potent anti-angiogenic activity (IC50=0.8 nM) and induces the collapse of newly formed capillary tubules.2 Modulates alternative splicing of VEGF in favor of anti-angiogenic isoforms.3 Induces apoptosis in ALL cell lines.4 Induces unfolded protein response in oral cancer cells.5 Cell permeable.
Biochemicals & reagents
7184-60-3
U-78548; C2989; Treponemycin
1) Ruan et al. (2005), A unique hydrophobic cluster near the active site contributes to differences in borrelidin inhibition among threonyl-tRNA synthetases; J. Biol. Chem., 280 571 / 2) Kawamura et al. (2003), Anti-angiogenesis effects of borrelidin are mediated throigh distinct pathways: threonyl-tRNA synthetase and caspases are independently involved in suppression of proliferation and induction of apoptosis in endothelial cells; J. Antibiot., 56 709 / Habibi et al. (2012), Borrelidin, a small molecule nitrile-containing macrolide inhibitor of threonyl-tRNA synthetase, is a potent inducer of apoptosis in acute lymphoblastic leukemia; Invest. New Drugs, 30 1361
-20°C
TARGET: RNA; UPR (Unfolded Protein Response); Antibiotic -- PATHWAY: Degradation; Apoptosis inducer; Protein synthesis; VEGF -- RESEARCH AREA: Ubiquitin/Proteasome; Angiogenesis; Cell death -- DISEASE AREA: Cancer; Infectious disease