Stone K J, Strominger J L
Proc Natl Acad Sci U S A. 1972 May;69(5):1287-9. doi: 10.1073/pnas.69.5.1287.
Bacitracin is an inhibitor of the biosynthesis of squalene and sterols from mevalonic acid, C(5)-isopentenyl pyrophosphate, or C(15)-farnesyl pyrophosphate catalyzed by preparations from rat liver. The antibiotic is active at extremely low ratios of antibiotic to substrate. The mechanism of inhibition appears to be the formation of a complex between bacitracin, divalent cation, and C(15)-farnesyl pyrophosphate and other isoprenyl pyrophosphates. It is similar to the formation of the complex with C(55)-isopropenyl pyrophosphate in microbial systems. The toxicity of bacitracin for animal cells could be due in part to the formation of these complexes.
杆菌肽是一种由大鼠肝脏制剂催化的、抑制从甲羟戊酸、C(5)-异戊烯基焦磷酸或C(15)-法尼基焦磷酸生物合成角鲨烯和甾醇的物质。该抗生素在抗生素与底物的比例极低时仍具有活性。抑制机制似乎是杆菌肽、二价阳离子与C(15)-法尼基焦磷酸及其他异戊二烯基焦磷酸形成复合物。这类似于在微生物系统中与C(55)-异丙烯基焦磷酸形成复合物的情况。杆菌肽对动物细胞的毒性可能部分归因于这些复合物的形成。