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. 1989 Aug 11;17(15):6339–6348. doi: 10.1093/nar/17.15.6339

Structure-activity relationships for the inhibition of DNA polymerase alpha by aphidicolin derivatives.

G Prasad 1, R A Edelson 1, P D Gorycki 1, T L Macdonald 1
PMCID: PMC318281  PMID: 2505232

Abstract

Aphidicolin and 17 derivatives that have been structurally modified in the A- and D-rings were assessed for their ability to inhibit DNA polymerase alpha. No derivative surpassed the activity of aphidicolin; derivatives with structural alterations in the A-ring exhibited significantly greater loss of activity relative to derivatives with structural alterations in the D-ring. The conclusions of these studies indicate a critical role for the C-18 function in the interaction of aphidicolin with polymerase alpha. Molecular modelling studies could not identify structural features of the aphidicolin-dCTP "overlap" that is unique to dCTP, relative to the remaining dNTPs, and that is consistent with the extant structure-activity data.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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