DNA-Interactive Drugs: U-77,779 (bizelesin)


 
 
Name U-77,779 
Bizelesin
MW 815.72
Category Cyclopropylpyrroloindole
Binding Mode Minor groove binding drug, forms covalent adduct to N3-A.
Site Specificity Crosslinks adenines on opposite strands of DNA, 6 to 7 bp apart.  Requires an A/T sequence, with a preference for runs of A [Lee, 1993].  In a favorable context, one end can adduct to guanine [Sun, 1993].
Effect on DNA Eliminates intrinsic bending of A/T-rich regions [Lee, 1993], stabilizes DNA in an unbent conformation [Thompson, 1995].
Preparation and Use Initial stock are prepared from powder, 2mg/mL in N,N dimethylacetamide.  Substock diluted to 2.5mM with DMSO.  Further dilutions are prepared with water.
 
DNA drugs
Heme-Onc
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Please direct all comments to: Jack Welch, M.D., Ph.D.
Last Modified August 1, 1998