Comments on: Src and Syk kinase attenuation of HIV infection http://walkerma.wordpress.com/2007/03/21/src-and-syk-kinase-attenuation-of-hiv-infection/ A medicinal chemist searching for that needle in a haystack Wed, 20 Aug 2008 12:00:44 +0000 http://wordpress.org/?v=MU By: Wavefunction http://walkerma.wordpress.com/2007/03/21/src-and-syk-kinase-attenuation-of-hiv-infection/#comment-229 Wavefunction Sat, 07 Apr 2007 13:52:21 +0000 http://walkerma.wordpress.com/2007/03/21/src-and-syk-kinase-attenuation-of-hiv-infection/#comment-229 Piceatonnol looks a <i>lot</i> like resveratrol the wine molecule. I wonder if res also inhibit these (or other) kinases. Piceatonnol looks a lot like resveratrol the wine molecule. I wonder if res also inhibit these (or other) kinases.

]]> By: walkerma http://walkerma.wordpress.com/2007/03/21/src-and-syk-kinase-attenuation-of-hiv-infection/#comment-216 walkerma Thu, 05 Apr 2007 16:32:55 +0000 http://walkerma.wordpress.com/2007/03/21/src-and-syk-kinase-attenuation-of-hiv-infection/#comment-216 Structure corrected...there were no structures, chemical-formulas or references given for PP2, so I had to rely on what SciFinder gave. Virology is my field, not kinases...even so, I would have like to see them use more-active/selective agents. The title of the paper promises more than the experiments were able to deliver. Structure corrected…there were no structures, chemical-formulas or references given for PP2, so I had to rely on what SciFinder gave.

Virology is my field, not kinases…even so, I would have like to see them use more-active/selective agents. The title of the paper promises more than the experiments were able to deliver.

]]> By: kinasepro http://walkerma.wordpress.com/2007/03/21/src-and-syk-kinase-attenuation-of-hiv-infection/#comment-215 kinasepro Thu, 05 Apr 2007 01:45:22 +0000 http://walkerma.wordpress.com/2007/03/21/src-and-syk-kinase-attenuation-of-hiv-infection/#comment-215 I don't know anything about CD4+ translation of the yadda yadda yadda, but far be it from me to let a blog entry on Kinase inhibitors go un-besmirched! I do pretend to know a thing or two about them in the chemblogosphere after all. So... Well... first fix structure plz: PP2 is ClC1=CC=C(C2=NN(C(C)(C)C)C3=C2C(N)=NC=N3)C=C1 Second... Hmmm well, paper's interesting I guess. I take it to say: kinases may be involved. But frankly - PP2 hits tons of kinases, mostly in the SRC family, but a number outside as well like ckit, and even abl, so isn't it a bit hard to make any conclusions about target? (not so much your conclusions, but those in the paper) Also piceatannol is only about 1 uM @ Km on SYK. I don't know anything about the selectivity of the latter - but certainly the non-kinase activity would be relevant to the article. I would put money on Ariad having some insanely selective SRC inhibitors and a collaboration using one of their compounds to investigate the theory would certainly be interesting... PP2? Umm... Not so much. Likewise with somebody like Rigel and SYK. I guess I'm just not impressed with their choice of inhibitors. Personally, I blame the French. I don’t know anything about CD4+ translation of the yadda yadda yadda, but far be it from me to let a blog entry on Kinase inhibitors go un-besmirched! I do pretend to know a thing or two about them in the chemblogosphere after all.

So… Well… first fix structure plz: PP2 is ClC1=CC=C(C2=NN(C(C)(C)C)C3=C2C(N)=NC=N3)C=C1

Second… Hmmm well, paper’s interesting I guess. I take it to say: kinases may be involved. But frankly - PP2 hits tons of kinases, mostly in the SRC family, but a number outside as well like ckit, and even abl, so isn’t it a bit hard to make any conclusions about target? (not so much your conclusions, but those in the paper) Also piceatannol is only about 1 uM @ Km on SYK. I don’t know anything about the selectivity of the latter - but certainly the non-kinase activity would be relevant to the article.

I would put money on Ariad having some insanely selective SRC inhibitors and a collaboration using one of their compounds to investigate the theory would certainly be interesting… PP2? Umm… Not so much. Likewise with somebody like Rigel and SYK. I guess I’m just not impressed with their choice of inhibitors.

Personally, I blame the French.

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