Document 0689 DOCN M9590689 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 SO NIH Conf Retroviral Integrase. 1995 Jan 19-20;:(Participants' abstracts and posters, abstract no. 9). Unique Identifier : AIDSLINE AIDS/95920030 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 Circular Dichroism Computer Simulation DNA Nucleotidyltransferases/*CHEMISTRY Enzyme Stability HIV-1/*ENZYMOLOGY Heat *Leucine Zippers Nuclear Magnetic Resonance Protein Conformation MEETING ABSTRACT SOURCE: National Library of Medicine. NOTICE: This material may be protected by Copyright Law (Title 17, U.S.Code).