Optimization of ligand affinity for rna targets using mass...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/68 (2006.01) C07H 19/056 (2006.01) G01N 27/00 (2006.01) G01N 33/483 (2006.01) H01J 49/10 (2006.01)

Patent

CA 2366488

The present invention provides methods for the identification ligand compounds that bind to target molecules such as proteins or structured RNA with as little as millimolar (mM) affinity using mass spectrometry. The methods may be used to determine the mode of binding interaction between two or more of these ligand compounds to the target as well as their relative affinities. Also provided are methods for designing compounds having greater affinity to a target molecule by identifying two or more ligands using mass spectrometry methods of the invention and linking the ligands together to form a novel compound.

L'invention concerne des procédés d'identification de composés de ligands se liant à des molécules cibles, notamment des protéines ou des ARN structurés avec une affinité de l'ordre du millimole (mM) faisant appel à la spectrométrie de masse. Ces procédés sont utilisés pour déterminer le mode d'interaction de liaison entre deux ou plusieurs composés de ligands avec la cible ainsi que leurs affinités relatives. Font aussi l'objet de cette invention des procédés de conception de composés présentant une affinité plus importante avec une molécule cible par identification de deux ligands au moins grâce à la spectrométrie de masse et de liaison des ligands entre eux afin d'obtenir un nouveau composé.

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