Document 0704
 DOCN  M9590704
 TI    The integrase proteins of HIV-1 and HIV-2: potential targets for
       anti-HIV drugs
 DT    9509
 AU    Plasterk RHA; Vink C; Puras-Lutzke R; van den Ent F; van der Linden K;
       The Netherlands Cancer Institute, Amsterdam (RPLAS@ron.nki.nl)
 SO    NIH Conf Retroviral Integrase. 1995 Jan 19-20;:(Session III, speakers'
       abstracts - unpaged). Unique Identifier : AIDSLINE AIDS/95920015
 AB    The mechanism of HIV DNA integration has been studied in vitro, using
       integrase protein purified from recombinant E. coli, and synthetic
       oligonucleotide substrates. Recent studies focus on structure/function
       analysis of integrase, using mutant derivatives of the protein. In
       parallel with these mechanistic studies we have taken two different
       approaches to find inhibitors of integrase: 1. We have further developed
       an assay previously developed by Craigie et al. (1991) and Mueller et
       al. (1994), to test integration activity in a microtiter assay. Our
       assay (Vink et al. 1994), employs a non-radioactive label instead of
       [32P], and is done within a single well of a microtiter plate (without
       transfer steps). This makes it more convenient for large scale screens.
       Recent progress will be presented. 2. We have tested Combinatorial
       Peptide Libraries (Houghten et al., 1991) and found peptides that
       inhibit integrase activity.
 DE    Antiviral Agents/METABOLISM/*PHARMACOLOGY  *DNA
       Nucleotidyltransferases/*METABOLISM  DNA, Viral/GENETICS
       HIV-1/*ENZYMOLOGY/GENETICS  HIV-2/*ENZYMOLOGY/GENETICS  Substrate
       Specificity  Virus Integration/GENETICS  MEETING ABSTRACT

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