Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:2.7.7.7 (DNA polymerase)
 17,007 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Bioassay-guided fractionation of an active methyl ethyl ketone extract of Tetracera boiviniana, using a sensitive assay to monitor DNA polymerase beta inhibition, resulted in the isolation of three known triterpenoids, betulinic acid (1), 3-cis-p-coumaroyl maslinic acid (2), and 3-trans-p-coumaroyl maslinic acid (3). Compounds 1-3 inhibited DNA polymerase beta with IC50 values of 14, 15, and 4.2 microM in the presence of bovine serum albumin (BSA) and 6.5, 7.5, and 2.0 microM in the absence of BSA, respectively. Further, compounds 1-3 potentiated the effects of bleomycin in cultured P-388D1 cells.
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PMID:DNA polymerase beta inhibitors from Tetracera boiviniana. 1065 14

DNA topoisomerases and DNA polymerases are enzymes that play a crucial role in DNA metabolism events such as replication, transcription, recombination, and chromosome segregation during mitosis. Thus, DNA topoisomerases and DNA polymerases inhibitors could be expected to have antitumor effects. Naturally occurring triterpenoids isolated from Junellia aspera (Gillies & Hook; Moldenke) (Verbenaceae) were assayed for human DNA topoisomerase I and Taq DNA polymerase inhibitory activities. Maslinic acid (2) and its diacetyl derivative (7) showed human DNA topoisomerase I inhibitory activity with IC50 values in the range of 76-80 microM and growth inhibition against various human solid tumour cell lines with GI50 values in the range of 5-18 microM. The triterpene frames could be used for screening new inhibitors of the enzyme, and computer-simulated drug design using the frame and pocket structure of enzyme may in theory be a possible approach to develop new inhibitors.
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PMID:Inhibition of DNA topoisomerase I and growth inhibition of human cancer cell lines by an oleanane from Junellia aspera (Verbenaceae). 1753 Nov 44