Conformationally constrained analogues of diacylglycerol (DAG). 14.1 Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharma cophore replacement

作者: Victor E. Marquez , Rajiv Sharma , Shaomeng Wang , Nancy E. Lewin , Peter M. Blumberg

DOI: 10.1016/S0960-894X(98)00307-2

关键词: Protein kinase C bindingProtein kinase CSulfonateChemistryLipid bilayerStereochemistryDiacylglycerol kinaseLigand (biochemistry)LactoneAlkyl

摘要: The replacement of the sn-1 and sn-2 carbonyl esters in DAG-surrogate lactones by sulfonate showed that their isosteric properties protein kinase C binding are controlled location hydrophobic alkyl chain on molecule. CO SO2 groups appear to be true isosteres only when they adjacent chain, which is presumed insert normal lipid bilayer.

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