Headpieces for dna-encoded chemical libraries
AssigneeUniversite de Montreal
InventorsMarc-Andre POUPART, Julien POUPART, Christian LE GOUILL, Antoine DOUCHEZ
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Abstract
The present document relates to headpieces for DNA-encoded chemical libraries and processes for preparing them, to DNA-encoded chemical libraries and DNA-supported pharmacophores or control molecules comprising the headpiece, and to uses thereof. The present document further relates to a method for generating multidimensional selection maps for a DNA-encoded library (DEL) (e.g., double-stranded or single-stranded DEL) against a single target.
Claims46
A headpiece, wherein said headpiece comprises a first polynucleotide sequence and a second polynucleotide sequence, wherein:
- said second polynucleotide sequence comprises a sequence that is complementary to the first polynucleotide sequence;
- at least part of said first and second polynucleotide sequences forms a double stranded polynucleotide sequence;
- said first and second polynucleotide sequences are covalently and irreversibly linked to each other through at least one modified base pair present in the double stranded polynucleotide sequence;
- and
- said first and second polynucleotide sequences each comprise a first and a second end, wherein:
- one of the first ends comprises a functionalizable moiety attached through a linker;
- the other of the first ends comprises a chain termination nucleotide;
- and
- the second ends comprise a DNA anchor site.
A headpiece, wherein said headpiece comprises a first polynucleotide sequence (e.g., sense strand) and a second polynucleotide sequence (e.g., antisense strand), wherein:
- said second polynucleotide sequence comprises a sequence that is complementary to the first polynucleotide sequence;
- at least part of said first and second polynucleotide sequences forms a double stranded polynucleotide sequence;
- said first and second polynucleotide sequences are covalently and irreversibly linked to each other through at least one modified base pair present in the double stranded polynucleotide sequence;
- and
- said first and second polynucleotide sequences each comprise a 5′- and a 3′-end, wherein:
- the 5′ end of the first polynucleotide sequence comprises a functionalizable moiety attached through a linker;
- the 5′ end of the second polynucleotide sequence comprises a chain termination nucleoside, preferably a dideoxynucleoside;
- the second polynucleotide sequence comprises one or more deoxy-uridine residues used as enzymatic cleavage sites;
- and
- the 3′ end of the first polynucleotide sequence comprises a two-nucleotide single strand overhang and the 5′ ends of the second polynucleotide sequence comprise a 5′-phosphate, thereby creating a DNA anchor site.
Dependencies are inferred from the claim text.