Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effectof constraining the glycerol backbone in DAG lactones

New synthetic diacylglycerols (DAGs) with equivalent branched acyl chains w ere 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 res ulted in a 10-fold increase in potency. Published by Elsevier Science Ltd.