AI Article Synopsis
- The study explored the role of the A-ring C(7) acetate in bryostatin 1 by creating and testing a new analogue with this feature in its structure.
- No improvement in the binding strength to protein kinase C (PKC) was found when compared to other analogues without the C(7) acetate.
- Biological tests indicated that the new analogue produced effects similar to phorbol ester PMA but different from the effects of bryostatin 1.
Article Abstract
The contribution of the A-ring C(7) 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 C(7) acetate. Functional assays showed biological responses characteristic of those induced by the phorbol ester PMA and distinctly different from those observed with bryostatin 1.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3075950 | PMC |
| http://dx.doi.org/10.1021/ol900585t | DOI Listing |
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