CA2245558A1 - Affinity labeling libraries and applications thereof - Google Patents

Abstract

Novel methods and compositions are provided for preferentially bonding an oligomeric molecule to a macromolecular target where the target is a member of a complex mixture and/or there is preferential bonding at one of a plurality of available bonding sites of the macro--molecular target. The methods represent a complete system for both producing and identifying affinity label molecules from a combinatorial library which preferentially bind to a macromolecular target or target site and preferentially binding those affinity labels to a macromolecule of interest either ex vivo or in vivo. Macromolecular targets include a variety of cellular- and non-cellular-associated proteins. Affinity la-bel molecules and combinatorial libraries thereof find use in providing means for inhibiting catalytic enzyme activity, accomplishing agonism and/or antagonism at biological receptor sites, attaching biologically active compounds to specific target sites in vivo, labeling macromolecules for premature destruction in vivo, directing biologically active com-pounds to specific sites in vivo and exploiting numerous sites that have been hitherto difficult to target, including tumorigenic-specific sites.