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- W4211070911 abstract "Abstract Integrase (IN) is one of only three viral enzymes encoded by the human immunodeficiency virus (HIV). The enzymatic activity of IN catalyzes the “integration” of viral double‐stranded DNA into host chromatin. Several steps including assembly, nuclear import, and gap repair are involved in the overall integration process, but two distinct biochemical steps are catalyzed by IN. The first step called 3′ processing allows for water to cleave the terminal dinucleotide on the respective ends of the viral DNA. The second discreet step called strand transfer facilitates the nicking of the host DNA by the recessed 3′ hydroxyl groups of the processed viral DNA. It is this second step of strand transfer that has been the focus of the bulk share of drug discovery efforts to date and the only step successfully inhibited by compounds that all fall into a class called two‐metal chelators. The science around the integrase enzyme is presented from a high‐level view of integration as part of the retroviral replication cycle through a molecular view of the biochemistry of the integration process involving nucleic acid strands. This chapter discusses inhibition of the strand transfer process and presents the two‐metal pharmacophore model and inhibitor design. The body of this work is focused on numerous classes of two‐metal chelation inhibitors of HIV‐1 integrase including several clinical candidates. The chapter concludes with a short survey of potential next‐generation compounds that have appeared in the literature through the end of 2008." @default.
- W4211070911 created "2022-02-13" @default.
- W4211070911 creator A5048833977 @default.
- W4211070911 date "2010-09-15" @default.
- W4211070911 modified "2023-09-29" @default.
- W4211070911 title "HIV Integrase" @default.
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