Centrifugally-enhanced method of determining ligand/target...

G - Physics – 01 – N

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G01N 33/53 (2006.01) C12Q 1/02 (2006.01) C12Q 1/68 (2006.01) C12Q 1/70 (2006.01) G01N 33/15 (2006.01) G01N 33/50 (2006.01) G01N 33/567 (2006.01)

Patent

CA 2365300

Centrifugation is used to induce and/or enhance binding between macromolecular targets and either small-molecule ligands or larger biomolecules as single entities or mixtures. With the enhanced binding, the method of the invention permits detection of ligands that bind to target substances and improve the design of ligands. The process relies on centrifugal force to establish a differential and selective concentration gradient between macromolecular therapeutic targets and the desired ligands. Once formed, the information about the self-sorting binding events is derived by analyzing the differential gradient of macromolecules and ligands in situ or by fractionating the gradient into individual samples for independent analysis. A variety of methods or combinations thereof, can be used to look for enhanced levels of bound ligands.

La centrifugation est utilisée pour induire et/ou améliorer la liaison entre des cibles macromoléculaires et des ligands à petites molécules ou de grandes biomolécules pris séparément ou mélangés. Grâce à cette amélioration, le procédé permet de détecter les ligands qui se lient aux substances cibles et qui améliorent la conception de ces ligands. Le processus se fonde sur la force centrifuge pour établir un gradient de concentration différentiel et sélectif entre les cibles thérapeutiques macromoléculaires et les ligands souhaités. Une fois formés, on obtient des informations relatives aux événements de liaison autosélective dérivées de l'analyse du gradient différentiel des macromolécules et des ligands in situ ou du fractionnement du gradient en échantillons individuels en vue d'une analyse indépendante. Une grande variété de procédés ou leur combinaison peuvent servir pour rechercher des taux améliorés de ligands liés.

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