KinasePro

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

What’s this I hear?

Posted by kinasepro on February 22, 2007

Is that the sweet sound of Kinase-Blogging Whistling in the Wind? Why yes, yes indeed it is.  (link to the original KP entry)

No covalent PDB’s available afaik, but for a little graphical perspective check out GW572016 (lapatinib) bound to EGF: 1XKK

O=S(CCNCC1=CC=C(C2=CC3=C(NC4=CC=C(OCC5=CC=CC(F)=C5)C(Cl)=C4)N=CN=C3C=C2)O1)(C)=O

The cystine in question is highlighted blue

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3 Responses to “What’s this I hear?”

  1. I am sitting here, reading this, thinking…is the only way to inactivate that thiol by covalent attachment to an inhibitor? Is anyone looking at methylating/ethylating agents (methoxypyridines? ethoxypyridines?)…have a vague recollection that this is how the toxoflavins work.

  2. sks said

    i am sitting here, reading this, thinking … how many visits does KP get a day.

  3. kinasepro said

    On the cystine covalent inhibitors: it seems to me that I’ll occasionally see an academic J Med Chem, but other then the ene or yne-amides, I’m not familiar with anything in use. Anybody else?

    On the hits / day… I get a bunch, but I have this sneaking suspicion most are from Milkshake hammering refresh as he waits on his rotovap :p

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