Gtpase inhibitors and methods of use and crystal structure...

C - Chemistry – Metallurgy – 12 – N

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C12N 9/14 (2006.01) A61K 31/506 (2006.01) A61K 45/06 (2006.01) A61P 9/10 (2006.01) A61P 25/28 (2006.01) A61P 35/00 (2006.01) C12N 9/99 (2006.01) C30B 7/00 (2006.01) C30B 29/58 (2006.01) C40B 30/02 (2006.01) G01N 23/20 (2006.01) G01N 33/53 (2006.01) C12Q 1/34 (2006.01)

Patent

CA 2617056

The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchange activity, along with uses for the compounds including screening for compounds which recognize Rac GTPase, and methods of treating pathological conditions associated or related to a Rho family GTPase, including Rac. The preferred embodiments also relate to methods of using such compounds, or derivatives thereof, e.g., in therapeutics, diagnostics, and as research tools.

L'invention concerne, dans des modes de réalisation préférés, des procédés et des compositions agissant sur l'activité de liaison GTP de membres des GTPases de la famille Rho, de préférence les Rac (Rac1, Rac2 et/ou Rac3), ces compositions contenant des composés qui modulent l'activité d'échange GTP/GDP. La présente invention porte également sur des utilisations de ces composés y compris le criblage de composés reconnaissant la GTPase Rac, et sur des méthodes pour traiter des états pathologiques associés ou liés à une GTPase de la famille Rho, y compris Rac. Dans des modes de réalisation préférés, l'invention concerne aussi des procédés pour utiliser de tels composés ou des dérivés desdits composés, par ex., pour la thérapie, le diagnostic et comme outils de recherche.

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