Nishida H, Sakakibara T, Aoki F, Saito T, Ichikawa K, Inagaki T, Kojima Y, Yamauchi Y, Huang L H, Guadliana M A
Central Research Division, Pfizer Pharmaceuticals Inc., Aichi, Japan.
J Antibiot (Tokyo). 1995 Jul;48(7):657-66. doi: 10.7164/antibiotics.48.657.
A new rapamycin producing culture was isolated and designated as Actinoplanes sp. N902-109. The addition of a cytochrome P-450 inhibitor and precursor feeding using this culture, and biotransformation approaches generated new rapamycin analogs with modifications at C-4, C-9, C-16, C-27, C-28 and/or C-39. The immunosuppressive activity of the resulting analogs was established in the mixed lymphocyte reaction assay.
一种新的产生雷帕霉素的培养物被分离出来，并命名为游动放线菌属N902-109。使用该培养物添加细胞色素P-450抑制剂并进行前体补料，以及生物转化方法产生了在C-4、C-9、C-16、C-27、C-28和/或C-39处有修饰的新雷帕霉素类似物。通过混合淋巴细胞反应试验确定了所得类似物的免疫抑制活性。
