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The Bryostatin 1 A-Ring Acetate is Not the Critical Determinant for Antagonism of Phorbol Ester-Induced Biological Responses

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journal contribution
posted on 04.06.2009, 00:00 by Gary E. Keck, Wei Li, Matthew B. Kraft, Noemi Kedei, Nancy E. Lewin, Peter M. Blumberg
The contribution of the A-ring C7 acetate to the function of bryostatin 1 has been investigated through synthesis and biological evaluation of an analogue incorporating this feature into the bryopyran core structure. No enhanced binding affinity for protein kinase C (PKC) was observed, relative to previously characterized analogues lacking the C7 acetate. Functional assays showed biological responses characteristic of those induced by the phorbol ester PMA and distinctly different from those observed with bryostatin 1.