Compounds and methods for the inhibition of protein-protein...

Details Compounds and methods for the inhibition of protein-protein... Compounds and methods for the inhibition of protein-protein...

C - Chemistry, Metallurgy

12

Q

C12Q 1/00 (2006.01) C07B 61/00 (2006.01) C12Q 1/68 (2006.01) C12Q 1/70 (2006.01) G01N 33/53 (2006.01) G01N 33/543 (2006.01) G01N 33/566 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2312913

Compounds having molecular weights of less than 1500 daltons that non- covalently interact with target proteins and covalently bond to target proteins at amino acid side chains that are not part of enzyme active sites, in which covalently bound portions of the compounds sterically block the binding of the target proteins to other proteins, are disclosed. The compounds react with forward reaction rates at least 100 times faster than the forward reaction rates at which the compounds bond to the side chains of the corresponding free amino acids under physiological conditions. Compositions including these compounds and methods for preparing these compounds are also disclosed.

Cette invention se rapporte à des composés de poids moléculaires inférieurs à 1500 daltons, qui interagissent de manière non covalente avec des protéines cibles et se lient par covalence à des protéines cibles au niveau de chaînes latérales d'acides aminés qui ne font pas partie des sites actifs de l'enzyme, dans lesquels les parties liées par covalence de ces composés bloquent par voie stérique la liaison des protéines cibles à d'autres protéines. Ces composés réagissent avec des vitesses de réaction d'avance au moins cent fois supérieures aux vitesses de réaction d'avance auxquelles les composés se lient aux chaînes latérales des acides aminés libres correspondants dans les conditions physiologiques. Des compositions contenant ces composés et des procédés de préparation de ces composés sont également présentés.

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