Differential inhibition of polymerase and strand-transfer activities of HIV-1 reverse transcriptase Article (Faculty180)

cited authors

  • Tillekeratne, L M; Sherette, Angela; Fulmer, Jennifer A; Hupe, Lynn; Hupe, Donald; Gabbara, Sam; Peliska, J A; Hudson, Rich A

description

  • A new class of inhibitors of HIV-1 reverse transcriptase obtained by the systematic structural simplification of epicatechin and epigallocatechin gallates are also shown here to inhibit DNA-strand-transfer, a process critical to the completion of the HIV-1-RT reproduction and to recombination-associated mutation of the virus. Up to 80-fold selectivity for DNA-strand-transfer inhibition over polymerase inhibition was observed for a defined subset of these agents. Such specific DNA-strand-transfer inhibitors may have important therapeutic potential.

publication date

  • 2002

start page

  • 525

end page

  • 8

volume

  • 12