Evans Gary B, Furneaux Richard H, Lewandowicz Andrzej, Schramm Vern L, Tyler Peter C
Carbohydrate Chemistry, Industrial Research Limited, P. O. Box 31310, Lower Hutt, New Zealand.
J Med Chem. 2003 Jul 17;46(15):3412-23. doi: 10.1021/jm030145r.
The aza-C-nucleosides, Immucillin-H and Immucillin-G, are transition state analogue inhibitors of purine nucleoside phosphorylase, a therapeutic target for the control of T-cell proliferation. Immucillin analogues modified at the 2'-, 3'-, or 5'-positions of the azasugar moiety or at the 6-, 7-, or 8-positions of the deazapurine, as well as methylene-bridged analogues, have been synthesized and tested for their inhibition of human purine nucleoside phosphorylase. All analogues were poorer inhibitors, which reflects the superior capture of transition state features in the parent immucillins.
氮杂-C-核苷Immucillin-H和Immucillin-G是嘌呤核苷磷酸化酶的过渡态类似物抑制剂，嘌呤核苷磷酸化酶是控制T细胞增殖的治疗靶点。已经合成了在氮杂糖部分的2'、3'或5'位或脱氮嘌呤的6、7或8位修饰的Immucillin类似物，以及亚甲基桥连类似物，并测试了它们对人嘌呤核苷磷酸化酶的抑制作用。所有类似物都是较差的抑制剂，这反映了母体Immucillin对过渡态特征的更好捕捉。
