Drug evolution concept in drug design : 2. Chimera method

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DOIResolve DOI: http://doi.org/10.2174/157340606776056214
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Pages175189; # of pages: 15
SubjectChimera method; drug design; drug library; pha; scaffold; para-aminobenzoic acid; building blocks; drug evolution; 4-aminobenzoic acid; animals; binding sites; chemistry, pharmaceutical; chimera; combinatorial chemistry techniques; drug design; drug evaluation, preclinical; salicylic acid; structure-activity relationship
AbstractThe drug evolution method represents a novel approach towards efficient rational drug design by implementing the drug evolution concept to the creation and development of general chemical libraries with the purpose of allowing the identification of drug candidates with improved odds and lesser costs than the traditional drug design strategies. As another example of successful translation of the biological evolution into chemical evolution, the chimera method comprises the grafting of selected building blocks, identified through a basic search within a drug library, onto the same substitution sites on a rationally chosen scaffold. The method allows the creation of a library containing both drugs and prospective drug candidates without any priorly required knowledge on the pursued disease or molecular target. Two libraries having scaffolds derived from para-aminobenzoic acid and salicylic acid have exemplified the application of the chimera method. The validation of the method has been achieved through the high number of recognized drugs within the library, which exhibit in the same time a wide variety of therapeutic activities and interact with a broad spectrum of molecular targets. The drug -enriched chimera libraries are expected to provide a highly efficient access to novel drug candidates whose unspecified therapeutic effects should be further revealed through high-throughput screening.
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AffiliationNRC Biotechnology Research Institute; National Research Council Canada
Peer reviewedNo
NRC number47487
NPARC number3539192
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Record identifiera3cdce56-7c86-4938-9fb3-a47d028f93a0
Record created2009-03-01
Record modified2016-05-09
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