Laurent A F, Dumont S, Poindron P, Muller C D
Département d'Immunologie, Immunopharmacologie et Pathologie, U.A. no. 491 du CNRS, Université Louis Pasteur de Strasbourg, Illkirch, France.
Exp Hematol. 1996 Jan;24(1):59-67.
Mycophenolic acid (MPA) is the active part of the corresponding morpholinoethyl ester pro-drug Mycophenolate Mofetil. MPA, an inhibitor of IMP dehydrogenase, depletes GTP and thereby suppresses transfer of mannose and fucose to proteins. Treatment of human monocytes with a clinically attainable concentration of MPA (10 microM) decreases their attachment to endothelial cells and to laminin, but not to type I collagen or fibronectin. Our results not only elucidate a major role of mannose/fucose residues in homing of monocytes on activated endothelium but also explain in part the beneficial effects of MPA in rheumatoid arthritis and organ graft rejection.
霉酚酸(MPA)是相应的吗啉代乙酯前药霉酚酸酯的活性成分。MPA作为肌苷单磷酸脱氢酶的抑制剂,会消耗鸟苷三磷酸(GTP),从而抑制甘露糖和岩藻糖向蛋白质的转移。用临床可达到的MPA浓度(10微摩尔)处理人单核细胞,会降低它们与内皮细胞和层粘连蛋白的附着,但不会降低与I型胶原或纤连蛋白的附着。我们的结果不仅阐明了甘露糖/岩藻糖残基在单核细胞归巢至活化内皮细胞过程中的主要作用,还部分解释了MPA在类风湿性关节炎和器官移植排斥反应中的有益作用。