KinasePro

Kinase Chemistry – Just a year and a half behind the times.

US20060270673

Posted by kinasepro on December 1, 2006

Hidy Ho Merck and Co., I’d say nice AKT inhibitors, but I notice you’re doing your xeno studies sub-q.

>> Update >> I’ve been looking at these for an aweful long time trying to figure how they bind to the kinase domain…  and wondering why I couldn’t fathom it, but as usual – KP is a little slow.  They are PH domain inhibitors and Merck has plenty of literature on the subject:

Merck’s AKT
WO  2006065601
WO  2006036395
WO  2005100356
WO  2005100344
WO  2006110638
WO  2006091395
WO  2006068796

*Bioorganic & Medicinal Chemistry Letters  (2005),  15(3),  761-764
*Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors.    Biochemical Journal  (2005),  385(2),  399-408.
*The Akt/PKB family of protein kinases: a review of small molecule inhibitors and progress towards target validation.    Current Topics in Medicinal Chemistry (2005),  5(2),  109-125.
*Tetrahedron Letters  (2005),  46(16),  2779-2782
*”Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors” Biochemical Journal  (2005),  385(2),  399-408
*Bioorganic & medicinal chemistry letters  (2005),  15(4),  905-9

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