Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 9, Issue 10, Pages 2543-2548Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(01)00054-2
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We have applied SELEX (Systematic Evolution of Ligands by EXponential enrichment), a combinatorial method that employs biopolymers for drug discovery, to identify single stranded DNA sequences able to bind L-Tyrosinamide, a simple mimic of Tyrosine, an amino acid essential to the catalytic activity of several enzymes of pharmaceutical interest. After 15 SELEX cycles using L-Tyrosinamide immobilized on an affinity chromatography column, the percentage of aptamers specifically eluted from the affinity column with free L-Tyrosinamide was 55% of the total. Aptamers were subcloned and sequenced, allowing the identification of a highly conserved consensus sequence, and showed a K-d value for L-Tyrosinamide of 45 muM. The identified aptamer sequence will constitute the basis for further in vitro evolution protocols and structure-based drug design. (C). 2001 Elsevier Science Ltd. All rights reserved.
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