Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 S. Limestone St., Lexington, Kentucky 40536, USA.
J Am Chem Soc. 2012 Nov 7;134(44):18181-4. doi: 10.1021/ja3081154. Epub 2012 Oct 29.
GilOII has been unambiguously identified as the key enzyme performing the crucial C-C bond cleavage reaction responsible for the unique rearrangement of a benz[a]anthracene skeleton to the benzo[d]naphthopyranone backbone typical of the gilvocarcin-type natural anticancer antibiotics. Further investigations of this enzyme led to the isolation of a hydroxyoxepinone intermediate, leading to important conclusions regarding the cleavage mechanism.
吉尔菌素 OII 已被明确鉴定为关键酶,负责执行关键的 C-C 键断裂反应,该反应导致独特的苯并[a]蒽骨架重排为苯并[d]萘并吡喃酮骨架,这是典型的吉尔沃菌素型天然抗癌抗生素。对这种酶的进一步研究导致了羟基氧杂环庚酮中间体的分离,这对裂解机制的重要结论。