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Archive for the ‘IRAK’ Category

Amgen ‘n’ IRAK-4

Posted by kinasepro on February 20, 2007

Irak-4? Yah I never heard of it either, but the IRAKs appear to be immunology targets for which Amgen is way out in front. They’ve got a nice paper in Structure, a Biorg. Med. Chem. Lett., and 2 PDB’s: 2NRU, 2NRY.

At first look I was mesmerized by the tyrosine gatekeeper but a second glance on looking over the recent CIP: US20070037803 shows something interesting.


they suggest as much in the BMCL. Read the rest of this entry »

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PDB Update

Posted by kinasepro on December 12, 2006

The highlight is GSK’s SB-590885 bound to B-Raf: 2FB8 (They describe the oxime as a phenol isostere)


Also, Amgen released the structurally interesting IRAK-4 bound to staurosporine (2NRY), and a benzimidazole inhibitor (2NRU). The Bioorg Med Chem Lett came out in March and the Xray is featured in this Structure paper.


The tyrosine gatekeeper is certainly different

Looks like there’s an indolinone lodged in today’s update as well. 2JAV replaces 2CL1, dunno why, probably some sort of refinement. NEK2 ne1?

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