Rational screening of oligonucleotide combinatorial libraries for drug discovery
Open Access
- 1 January 1993
- journal article
- Published by Oxford University Press (OUP) in Nucleic Acids Research
- Vol. 21 (8) , 1853-1856
- https://doi.org/10.1093/nar/21.8.1853
Abstract
Combinatorial strategies offer the potential to generate and screen extremely large numbers of compounds and to Identify Individual molecules with a desired binding specificity or pharmacological activity. We describe a combinatorial strategy for ollgonucleotides In which the library is generated and screened without using enzymes. Freedom from enzymes enables the use of ollgonucleotlde analogues. This dramatically extends the scope of both the compounds and the targets that may be screened. We demonstrate the utility of the method by screening 2′-O-Methyl and phos-phorothioate oligonucleotlde analogue libraries. Compounds have been Identified that bind to the activated H-ras mRNA and that have potent antiviral activity against the human herpes simplex virus.Keywords
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