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Microarray Compound Screening (µARCS) to Identify Inhibitors of HIV Integrase

Department of Biological Screening, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

Tim Middleton

Infectious Disease Research, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

Debra Montgomery

Infectious Disease Research, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

Hock Ben Lim

Infectious Disease Research, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

Warren Kati

Infectious Disease Research, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

Akhter Molla

Infectious Disease Research, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

Xiaoling Xuei

Department of Biological Screening, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

Usha Warrior

Department of Biological Screening, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

James L. Kofron

Department of Biological Screening, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

David J. Burns

Department of Biological Screening, Abbott Laboratories, Global Pharmaceutical Products Division, Abbott Park, IL

A novel high-throughput strand transfer assay has been developed, using Microarray Compound Screening (µARCS) technology, to identify inhibitors of human immunodeficiency virus (HIV) integrase. This technology utilizes agarose matrices to introduce a majority of the reagents throughout the assay. Integration of biotinylated donor DNA with fluorescein isothiocyanate (FITC)-labeled target DNA occurs on a SAM membrane in the presence of integrase. An anti-FITC antibody conjugated to alkaline phosphatase (AP) was used to do an enzyme-linked immunosorbent assay with the SAM. An agarose gel containing AttoPhos, a substrate of AP, was used for detection of the integrase reactions on the SAM. For detection, the AttoPhos gel was separated from the SAM after incubation and then the gel was imaged using an Eagle Eye II closed-circuit device camera system. Potential integrase inhibitors appear as dark spots on the gel image. A library of approximately 250,000 compounds was screened using this HIV integrase strand transfer assay in µARCS format. Compounds from different structural classes were identified in this assay as novel integrase inhibitors.

Journal of Biomolecular Screening, Vol. 7, No. 3, 259-266 (2002)
DOI: 10.1177/108705710200700309


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