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August 14, 2002
Our Friend the Phosphate Group, Redux
By the way, just to introduce some medicinal chemistry into this week's postings, I should point out that there's another way in which kinases outnumber phosphatases: the number of inhibitors known. It's true that we went a long time without good structural classes of compounds to inhibit kinases, but the dam burst some years back.
Now we've beaten several classes of heterocyclic structures completely into the ground, and the patent landscape looks like Yasgur's farm after they got finished holding Woodstock. But we do have kinase inhibitors, and plenty of 'em. So where are the phosphatase blockers?
Look around the literature, and you see all sorts of odd and funky structures, but no unifying themes. The first outfit that finds a general drug-friendly structural template to go after these targets will have quite a franchise on its hands.
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