J Med Chem Review
Posted by kinasepro on January 10, 2007
If you subscribe to the J Med Chem feed, you’ve probably already seen this ‘perspective’. May I just say that rarely does a journal article have such a deep impact on me, but this one really shakes it up.
First thing I noticed was that he got the structure for Gleevec wrong. That right there told me to stop reading… But hey, where’s the fun in that?
Since some goofeballs actually read this blog, maybe I should be nice… Hmm….. Nah. Welcome to the internet age where you submit a halfbaked manuscript to a major journal and we prepare the flames.
None more then KP appreciate a good discussion on structural biology and kinase inhibitors, and I respect what the author is trying to accomplish here. It’s exceedingly difficult to represent and discuss a 3D model on 2D media. Being the managing editor of KinasePro I’ve experienced this first hand.
On the structures: “Triazolopyrimidine derivative (24)“: Wrong tautomer? Extra atoms? Missing Bonds? Wrong compound. “Compound 18 (AP23464)“: missing a bond. dasatinib is bis-protonated? purvalanol a is isopropyl not t-butyl, and of course in Gleevec the piperazine should be para not meta.
You could argue all this is really just book-keeping. More important is the content, and on that topic I have less to say. Perhaps this ‘perspective’ will further advance someones understanding of how inhibitors bind to kinases, maybe it wont, but doesn’t there come a time when during the course of the manuscript preparation you just have to take a step back and say…
this looks like crap ?
This (free link) article does a better job on the topic, but frankly there are subtleties that 2D and even 3D will just not access. Kudos to the author for approaching a difficult topic. Shame on J Med Chem for not properly
rejecting reviewing this offering. Oh, and Duke sucks.
>> Update 2/1/07 >> It looks as though J Med Chem finally made the corrections pointed out above. It will be interesting to see if the errors made it to print. I’m still not convinced (24) is the correct structure though.