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ID: ALA1133036
Journal: Bioorg Med Chem Lett
Title: Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.
Authors: Nacro K, Bienfait B, Lewin NE, Blumberg PM, Marquez VE.
Abstract: New synthetic diacylglycerols (DAGs) with equivalent branched acyl chains were compared with commercially available DAGs as PK-C ligands. The results support the view that there is a minimal lipophilic requirement provided by the equivalent acyl groups that results in high binding affinity. Locking the glycerol backbone of the most potent DAG into a five-member lactone resulted in a 10-fold increase in potency.
CiteXplore: 10762046