SYNTHESIS AND BIOLOGICAL-ACTIVITY OF SOME 2' DERIVATIVES OF ADENOSINE 3',5'-CYCLIC PHOSPHATE
SYNTHESIS AND BIOLOGICAL-ACTIVITY OF SOME 2' DERIVATIVES OF ADENOSINE 3',5'-CYCLIC PHOSPHATE
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DOI：
10.1021/bi00729a035
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发表时间：
1973-01-01
期刊：
影响因子：
2.9
通讯作者：
SIMON, LN
中科院分区：
文献类型：
--
作者：
MILLER, JP;SHUMAN, DA;SIMON, LN
Jon P.米勒，* Dennis A. Shuman，Mieka B. Scholten，玛丽K.作者：Charles M.斯图尔特，塔斯尼姆A.罗兰·赫瓦贾罗宾斯和莱昂内尔N.西蒙摘要：本文合成了一系列环腺苷酸（cAMP）的2 ′端衍生物，并通过研究它们作为cAMP磷酸二酯酶的底物和抑制剂以及激活cAMP依赖性蛋白激酶的能力，研究了它们的体外生物学性质。未封闭的核糖体构型的2 ′-OFI是cAMP激活蛋白激酶所必需的。2 '-D-取代衍生物和2'-脱氧-cAMP是较好的底物，
Jon P. Miller,* Dennis A. Shuman, Mieka B. Scholten, Mary K. Dimmitt, Charles M. Stewart, Tasneem A. Khwaja, Roland K. Robins, and Lionel N. Simon abstract: A series of 2'derivatives of cAMP were synthe-sized and their biological propertiesin vitro were investigated by studying their ability to serve as substrates for and inhibitors of cAMP phosphodiesterases, and to activate cAMP-depen-dent protein kinases. The unblocked 2'-OFI in the ribo con-figuration was found to be necessary for the activation of protein kinase by cAMP. 2'-D-Substituted derivativesand 2'-deoxy-cAMP were relatively good substrates for and in-