Morpholino-subunit combinatorial library and method
AssigneeAntivirals Inc.
InventorsJames E. Summerton, Dwight D. Weller
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Abstract
A method of generating a compound capable of interacting specifically with a selected macromolecular ligand is disclosed. The method involves contacting the ligand with a combinatorial library of oligomers composed of morpholino subunits with a variety of nucleobase and non-nucleobase side chains. Oligomer molecules that bind specifically to the receptor are isolated and their sequence of base moieties is determined. Also disclosed is a combinatorial library of oligomers useful in the method and novel morpholino-subunit polymer compositions.
Claims14
A combinatorial library of oligomers, each formed of at least four linked morpholino subunits of the form:
- ##STR4## in which (i) morpholino subunit structures are linked together by linkages L one to four atoms long joining the morpholino nitrogen of one subunit to the 4' cyclic carbon of an adjacent subunit, (ii) X.sub.i is a side chain in subunit i in each oligomer of the library, (iii) the different oligomers in the library have different sequences of side chains in at least three subunit positions, (iv) X.sub.i is selected from the group consisting of purines, pyrimidines, non-nucleobase aromatic side chains, aliphatic side chains, and mixed aromatic/aliphatic moieties, and (v) said library contains at least 1,000 different side chain sequence oligomers.
A composition of oligomers, each formed of at least four linked morpholino subunits of the form:
- ##STR7## in which (i) morpholino subunit structures are linked together by one-atom linkages joining the morpholino nitrogen of one subunit to the 4' cyclic carbon of an adjacent subunit, (ii) X.sub.i is a side chain in subunit i in each oligomer of the composition, (iii) the different oligomers in the composition have different sequences of side chains in at least three subunit positions, and (iv) X.sub.i is selected from the group consisting of purines, pyrimidines, non-nucleobase aromatic side chains, aliphatic side chains, and mixed aromatic/aliphatic moieties.
A composition of oligomers, each formed of at least four linked morpholino subunits of the form:
- ##STR8## in which (i) morpholino structures are linked together by carbanoyl-containing linkages joining the morpholino nitrogen of one subunit to the 4' cyclic carbon of an adjacent subunit, (ii) X.sub.i is a side chain in subunit i in each oligomer of the composition, (iii) the different oligomers in the composition have different sequences of side chains in at least three subunit positions, and (iv) X.sub.i is selected from the group consisting of purines, pyrimidines, non-nucleobase aromatic side chains, aliphatic side chains, and mixed aromatic/aliphatic moieties.
Dependencies are inferred from the claim text.