Generation and screening of a dynamic combinatorial library

摘要

The present invention concerns a method for selectively establishing a dynamic combinatorial library of ligands binding to a target which binds at least two functionalities, which method comprises the following steps: selecting a plurality of functionalities which upon combination with each other are capable of forming an antity which may bind to the at least two functionalities in the target; linking at least two identical or different functionalities by at least one spacer group allowing reversible bond formation, thus creating discrete ligands; mixing together a plurality of a different discrete ligands having different combinations of functionalities; subjecting the mixture to conditions allowing a reversible bond formation and cleavage, hence a scrambling of the formalities; analyzing the mixture obtained; adding the target to the mixture; again analyzing the mixture, comparing the results obtained and identifying the functionality combinations which are most appropriate for the formation of a bond. In a further embodiment of the invention, the target is added when the discrete ligands are mixed together, in order to be present when the scrambling takes place.