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Assay platform for screening and identifying allosteric and catalytic site inhibitors of viral polymerases.
Author(s) -
Gregory Kalvin,
Sun Ye,
Golovlev Val
Publication year - 2009
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.23.1_supplement.895.1
Subject(s) - polymerase , rna , dna polymerase , reverse transcriptase , allosteric regulation , chemistry , dna , computational biology , high throughput screening , drug discovery , enzyme , microbiology and biotechnology , virology , biology , biochemistry , gene
An assay platform consisting of two luminescent‐based assays has been developed for screening inhibitors of viral polymerases and for studying mechanisms of action of the prospective pharmaceutical compounds. The assays from this platform are designed to measure the activity of DNA‐directed DNA polymerases, RNA‐directed DNA polymerases, and RNA‐directed RNA polymerases, and can be used for identifying the mechanism of action of a prospective viral polymerase inhibitor in a single volume experiment and operating in real‐time detection mode. The assays have been demonstrated for detection of allosteric vs. catalytic site inhibition (e.g., NNRTI vs. NRTI) of HIV‐1 reverse transcriptase and for the study of the inhibition of RNA‐directed RNA polymerases. The assay platform addresses the drawbacks of the existing methods in that it reduces the cost of reagents and reduces the assay time. The technology is adaptable to high‐throughput format for application in large and small scale drug discovery projects.