3,5 CYCLIC NUCLEOTIDE PHOSPHODIESTERASES

在真核细胞中，许多信号通路使用 磷酸二酯酶，降解第二信使cAMP和cGMP。 PDES(3‘，5’环核苷酸磷酸二酯酶)降解cGMP或cAMP 到5‘一磷酸核苷酸。到目前为止，还没有任何PDE的结构 已有报道称。PDE2A1的36kD活性蛋白水解性片段 从牛脑中提取的(钙调蛋白刺激的PDE)已经结晶。 该活性片段包含整个~250残基催化 在9个PDE家族中发现了一致的序列。立方的i23 用非特异性PDE抑制剂IBMX生长晶体 (3-异丁基-1-甲基黄嘌呤)。观察到了4E的衍射峰 在公司内部。

In eukaryotic cells, many signaling pathways use phosphodiesterases, which degrade the second messengers cAMP and cGMP. PDEs (3',5' cyclic nucleotide phosphodiesterases) degrade cGMP or cAMP to the 5' monophosphate nucleotide. To date, no structure for any PDE has been reported. An active, 36 kD proteolytic fragment of PDE2A1 (calmodulin-stimulated PDE) from bovine brain has been crystallized. This active fragment contains the entire ~250 residue catalytic consensus sequence found among the 9 PDE families. The cubic I23 crystals are grown with the nonspecific PDE inhibitor IBMX (3-isobutyl-1-methylxanthine). Diffraction to 4 E has been observed in-house.