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


Posted by kinasepro on October 12, 2006

Guten Tag Schering AG,

Nice antibacterial you’ve got there posing as a kinase inhibitor. It seems like there’s a handful of these thiazolidinone PLK1 patent applications floating around. This offering from Schering isn’t their first of the series (WO2003093249, WO2005042505, WO2006082107) but it will be the first to get Kinasepro’s meat cleaver approach to figuring out how it’s binding. All Schering’s applications embody matter around the thiazolidinone core, with some subtle some not-so-subtle changes to the pendant functional groups.

To the best of KP’s knowledge there are no published Xrays of the kinase domain. It was looking like MIT had a patented one until you read the fine print and find its only another of the ‘polo-box-domain’ Pshaw Acadamics. Schering has a patent application on using a homology model for making these suckers, so don’t you even think about using this at home kids.

So what I’m getting at is that this is really just a guess, if there’s something public that your aware of that could help my understanding please feel free to chime in.

2 Responses to “WO2006063806”

  1. del said

    have you thought about revisiting this in light of the pfizer biochemistry paper?

  2. kinasepro said

    good idea, I think I had the right general idea but the alkyne might sit in a lypophillic crevice next to a cystine residue – under the glycine loop rather then H1…

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