Structure-activity relationships for the inhibition of DNA polymerase alpha by aphidicolin derivatives.
AUTOR(ES)
Prasad, G
RESUMO
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.
ACESSO AO ARTIGO
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=318281Documentos Relacionados
- Inhibition of DNA polymerase alpha by aphidicolin derivatives.
- Structure–Activity Relationships and Quantitative Structure–Activity Relationships for Breast Cancer Resistance Protein (ABCG2)
- Structure-activity relationships of the fluoroquinolones.
- Semisynthetic Coumermycins: Structure-Activity Relationships
- Structure-activity relationships of new antiviral compounds.