Methods for identifying ligand binding sites in a biomolecule

C - Chemistry – Metallurgy – 12 – Q

Patent

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C12Q 1/68 (2006.01) C07H 19/00 (2006.01) C07H 21/00 (2006.01) C07H 21/02 (2006.01) C07H 21/04 (2006.01) G01N 33/53 (2006.01) G01N 33/566 (2006.01) G01N 33/567 (2006.01)

Patent

CA 2439085

Methods of identifying ligand binding sites in a target molecule such as a polynucleotide or polypeptide, as well as methods for determining whether a particular site in a target molecule is at or near the ligand binding site, are provided. Ligand binding affinities corresponding to both the target molecule and a modified version thereof are compared, preferably using mass spectral analysis. The modified molecules, or test molecules, incorporate a modification capable of modulating ligand binding affinity when located at or near the ligand binding sites. Binding site information is derived from the known position of the modification.

L'invention concerne des procédés pour identifier des sites de liaisons aux ligands dans une molécule cible telle qu'un polynucléotide ou un polypeptide, ainsi que des procédés pour déterminer si un site particulier dans une molécule cible se trouve au niveau du site de liaison aux ligands ou proche de ce dernier. Des affinités de liaison aux ligands correspondant à la fois à la molécule cible et à une version modifiée de celle-ci sont comparées, de préférence à l'aide d'une analyse spectrale de masse. Les molécules modifiées, ou molécules test, comprennent une modification capable de moduler une affinité de liaison aux ligands lorsque cette modification est située au niveau des sites de liaison aux ligands ou proche de ceux-ci. Des informations concernant les sites de liaison sont dérivées de la position connue de la modification.

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