Conformationally constrained analogues of diacylglycerol (DAG).: 14.: Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement
Conformationally constrained analogues of diacylglycerol (DAG).: 14.: Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement
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DOI：
10.1016/s0960-894x(98)00307-2
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发表时间：
1998-07-07
影响因子：
2.7
通讯作者：
Lee, J
中科院分区：
文献类型：
--
作者：
Marquez, VE;Sharma, R;Lee, J
用磺酸酯取代DAG-替代内酯中的sn-1和sn-2羰基酯表明，它们在蛋白激酶C结合中的电子等排性质受分子上疏水烷基链的位置控制。CO和SO2基团似乎是真正的电子等排体，只有当它们是相邻的烷基链，这是假定插入正常的脂质双层。出版社：Elsevier Science Ltd
The replacement of the sn-l and sn-2 carbonyl esters in DAG-surrogate lactones by sulfonate esters showed that their isosteric properties in protein kinase C binding are controlled by the location of the hydrophobic alkyl chain on the molecule. The CO and SO2 groups appear to be true isosteres only when they are adjacent to the alkyl chain, which is presumed to insert normal to the lipid bilayer. Published by Elsevier Science Ltd.