Borrelidin is an unusual nitrile-containing metabolite isolated from Streptomyces. Borrelidin is an important lead for antimalarial discovery, displaying activity against drug-resistant Plasmodia.
Borrelidin is soluble in ethanol, methanol, DMF and DMSO.
Borrelidin is soluble in ethanol, methanol, DMF and DMSO.
| Mechanism of Action | Borrelidin is a selective inhibitor of bacterial and eukaryal threonyl-tRNA synthetase and is a very potent angiogenesis inhibitor and induces apoptosis of the capillary tube-forming cells. |
| References | A unique hydrophobic cluster near the active site contributes to differences in borrelidin inhibition among threonyl-tRNA synthetases. Ruan T. et al. , J. Biol. Chem. 2005, 280, 571. Borrelidin is an angiogenesis inhibitor; disruption of angiogenic capillary vessels in a rat aorta matrix culture model. Wakabayashi T. et al. , J. Antibiot. 1997, 50, 671. Anti-angiogenesis effects of borrelidin are mediated through distinct pathways: threonyl-tRNA synthetase and caspases are independently involved in suppression of proliferation and induction of apoptosis in endothelial cells. Kawamura T. et al. , J. Antibiot. 2003, 56, 709. |