Fragment-based design of ligands targeting a novel site on the integrase enzyme of human immunodeficiency virus 1

Jerome Wielens, Stephen Headey, John Deadman, David Rhodes, G Le, Michael Parker, David Chalmers, Martin Scanlon

Research output: Contribution to journalArticleResearchpeer-review

26 Citations (Scopus)


The genome of the human immunodeficiency virus (HIV) encodes three enzymes that are essential for viral replication. Of these, the integrase (IN) enzyme remains significantly underexploited as a therapeutic target although clinically, inhibition of IN has been demonstrated to reduce viral load in HIV-1-infected individuals.[1] During the HIV replication cycle, IN catalyzes two reactions.[2] In the first, IN binds pro-viral cDNA in the host-cell cytoplasm and catalyzes the removal of two conserved nucleotides (GT) from the 3 -ends of the long terminal repeat (LTR) strands. Following 3 processing, the pre-integration complex (PIC) is transported into the nucleus where the second reaction-strand- transfer-occurs.
Original languageEnglish
Pages (from-to)258 - 261
Number of pages4
Issue number4
Publication statusPublished - 2011

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