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This version was published on June 1, 2008
Journal of Biomolecular Screening, Vol. 13, No. 5, 406-414 (2008)
DOI: 10.1177/1087057108317060

Screening for Antiviral Inhibitors of the HIV Integrase—LEDGF/p75 Interaction Using the AlphaScreenTM Luminescent Proximity Assay

Yan Hou

Department of Virology, Schering-Plough Research Institute

Debra E. Mcguinness

Department of New Lead Discovery, Schering-Plough Research Institute

Andrew J. Prongay

Department of Chemical Research, Schering-Plough Research Institute, Kenilworth, New Jersey

Boris Feld

Department of Virology, Schering-Plough Research Institute

Paul Ingravallo

Department of Virology, Schering-Plough Research Institute

Robert A. Ogert

Department of Virology, Schering-Plough Research Institute

Charles A. Lunn

Department of New Lead Discovery, Schering-Plough Research Institute

John A. Howe

Department of Virology, Schering-Plough Research Institute, john.howe{at}spcorp.com

Small-molecule inhibitors of HIV integrase (HIV IN) have emerged as a promising new class of antivirals for the treatment of HIV/AIDS. The compounds currently approved or in clinical development specifically target HIV DNA integration and were identified using strand-transfer assays targeting the HIV IN/viral DNA complex. The authors have developed a second biochemical assay for identification of HIV integrase inhibitors, targeting the interaction between HIV IN and the cellular cofactor LEDGF/p75. They developed a luminescent proximity assay (AlphaScreenTM) designed to measure the association of the 80-amino-acid integrase binding domain of LEDGF/p75 with the 163-amino-acid catalytic core domain of HIV IN. This assay proved to be quite robust (with a Z' factor of 0.84 in screening libraries arrayed as orthogonal mixtures) and successfully identified several compounds specific for this protein-protein interaction. (Journal of Biomolecular Screening 2008:406-414)

Key Words: HIV integrase • LEDGF/p75 • protein-protein interaction • AlphaScreen • orthogonal mixtures


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