A method for the generation of a dynamic combinatorial library

摘要

The present invention relates to a method of forming a dynamic library of compounds which are potentially capable of binding to a target, which method comprises i) selecting one first set of molecules which molecules each carry at least one first functional group which is capable of interacting with at least one other functional group under the formation of reversible bonds; ii) selecting at least one further set of molecules which molecules carry at least one second functional group which is capable of interacting with the first functional group on the first set of molecules; iii) reacting the two sets of molecules with each other and at least temporarily in the presence of the target, under conditions where a formation of reversible bonds between the functional groups on the molecules forming each of the sets occurs; wherein the formation of the library occurs under physiological conditions and is fully reversible throughout the entire formation of the library, and the respective amounts of each set of molecules employed are such that one functional group of that at least first and second functional groups is present in a large excess with respect to the other functional group during the formation of the library. ??Pharmaceutically active compounds which are formed when the library is generated can be identified by analysing the library, preferably by comparing the amounts of the compounds formed in the presence of the target and in the absence of the target. ??The method according to the invention permits to form library which are fully operative throughout their entire process of formation, i.e. the reactions leading to the components of the library take place in the entire process of generating and screening the library.