PMID: 2505232Aug 11, 1989Paper

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

Nucleic Acids Research
G PrasadT L Macdonald

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.

References

Jul 25, 1979·Nucleic Acids Research·M LongiaruM S Horwitz
Jun 10, 1988·Nucleic Acids Research·L ArabshahiG Wright
Apr 1, 1985·Antiviral Research·S SpadariG Pedrali-Noy
Oct 1, 1984·Journal of Medicinal Chemistry·J E McMurry, T R Webb
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May 1, 1984·Journal of Natural Products·J Ipsen, J P Rosazza
Feb 1, 1981·Journal of Biochemical and Biophysical Methods·G Pedrali-NoyS Spadari

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Citations

Jan 1, 1990·Pharmacology & Therapeutics·G E Wright, N C Brown
Dec 20, 2000·Antimicrobial Agents and Chemotherapy·O KayserK Siems
Nov 29, 2014·Nucleic Acids Research·Andrey G BaranovskiyTahir H Tahirov
Feb 18, 2017·Genes·Andrey G Baranovskiy, Tahir H Tahirov
Sep 3, 1991·Biochemistry·R SheaffR Kuchta
May 18, 2016·Nature Chemical Biology·Ting HanDeepak Nijhawan

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