Physical Sciences and Mathematics Commons^™

Binding Properties Of Large Antiviral Polyamides (Pa1 And Pa25) And Natural Product Derivatives As Inhibitors Of Serine Hydrolases, Elena Vasilieva

Dissertations

Polyamides are a class of DNA minor groove binders that were developed from the natural product Distamycin A. PA25 (20-ring PA) showed better activity (3-fold) in the elimination of HPV16 episomes than PA1 (14-ring PA). Binding studies of PA1 and PA25 were performed in the long control region of HPV16 (7348-122 bp). PA1 showed similar binding affinity to perfect match and single mismatch binding sites. PA1 bound to double, triple, and quadruple mismatch sites with lower affinity. PA25 bound with similar binding affinity to perfect through triple mismatch binding sites. PA25 bound quadruple mismatch sites and nonspecifically. Therefore, it was …