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Bioorg Med Chem Lett. 2000 Apr 3;10(7):653-5.

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.

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1
Laboratories of Medicinal Chemistry, Division of Basic Sciences, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.

Erratum in

  • Bioorg Med Chem Lett 2000 Jun 19;10(12):1401.

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.

PMID:
10762046
DOI:
10.1016/s0960-894x(00)00070-6
[Indexed for MEDLINE]

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