Structures of substrate binding pockets of scf complexes

C - Chemistry – Metallurgy – 12 – N

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C12N 9/00 (2006.01) A61K 45/00 (2006.01) G01N 23/20 (2006.01) G01N 33/53 (2006.01) G06F 17/00 (2006.01) G06F 17/50 (2006.01) G06F 19/00 (2006.01)

Patent

CA 2443370

The present invention relates to binding pockets of Skpl-Cdc53/Cullin-F-box protein (SCF) E3 ubiquitin ligases associated with substrate selection and/or orientation. In particular, the invention relates to a crystal comprising such binding pockets. The crystal may be useful for modeling and/or synthesizing mimetics of a binding pocket or ligands that associate with the binding pocket. Such mimetics or ligands may be capable of acting as modulators of the interactions of a SGF E3 ubiquitin ligase and its substrates, and they may be useful for treating, inhibiting, or preventing diseases modulated by such interactions. Methods are also provided for regulating a SCF E3 ubiquitin ligase comprising changing a binding pocket associated with substrate selection and/or orientation.

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