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Posts tagged with "Pharmacokinetics"

  • Chemical Biology

    Curcumin Will Waste Your Time

    I really enjoyed reading this article in J. Med. Chem. on curcumin. (Update: here’s the take over at Practical Fragments). That’s a well-known natural product, found in large quantities in turmeric root (which is where most of the yellow color comes from). It has, over the years, been a hit in many, many assays, and… Read More
  • Alzheimer's Disease

    A New Way to Make GSK3 Inhibitors

    Of the discovery of GSK3 (glycogen synthase kinase 3) inhibitors there has been no end. I first came across it as a target it about 1997, and even then, once I started reading the literature, I quickly felt as if I were late to the party. It’s been investigated for diabetes (and other metabolic diseases), Alzheimer’s… Read More
  • "Me Too" Drugs

    Isotope Labeling For Fun and Profit

    Here’s an article on a company called Molecular Isotope Technologies, and their bid to “revolutionize the drug industry”. From the name, you might expect that this is another deuterium-for-proton idea, and you would say to yourself “But that’s already been done”. But read on. The company is perhaps better known b… Read More
  • Cancer

    Nanoparticles Mix It Up With Reality

    Nanoparticles (well, papers about nanoparticles) have been impossible to avoid for. . .what, ten years now, would you say? There’s so much potential there in so many fields, and there are so many things to try, that the literature is a gigantic pile that gets more deliveries dumped on it every week. And how many… Read More
  • Animal Testing

    A Terrific Paper on the Problems in Drug Discovery

    Here’s a really interesting paper from consultants Jack Scannell and Jim Bosley in PLoS ONE, on the productivity crisis in drug discovery. Several things distinguish it: for one, it’s not just another “whither the drug industry” think piece, of which we have plenty already. This one get quantitative, attempting to figure out… Read More
  • Drug Assays

    Park Your Drug Right Here For a While

    Here’s a ten-year look back at the whole concept of residence times in drug discovery, published by Bob Copeland of Epizyme in Nature Reviews Drug Discovery. He’s the one to write it, since he’s one of the key developers of the whole concept, which certainly seems to have made a home for itself in the… Read More
  • Chemical News

    Cubane to the Rescue

    Medicinal chemists are interested in weird ring systems – I can’t deny it. We like them for several reasons, one of which is that we’re always looking for variations on structural themes that might affect the metabolism or absorption of our drug molecules. And the fact that these variations can lead to new patentable chemical… Read More
  • Drug Development

    More 3-D Drug Printing Excitement

    Chemjobber drew my attention to this a few days ago, rightly noting that someone was indeed falling for a big ol’ pile of hype. There’s an awful lot of breathless stuff out there about “3-D printed drugs”, and this will serve as a fine example. Many of these pieces suffer from one or more of… Read More
  • Cancer

    Another Funny-Looking Structure Comes Through

    Here’s one that I certainly wouldn’t have thought about doing. This recent paper in ACS Medicinal Chemistry Letters describes changing the substituents off the core of a PAK1 inhibitor. Nothing too interesting about that, you’d think: the inhibitor itself is one of your standard-looking kinase inhibitor sausage strings of heteroar… Read More
  • Cancer

    Blasting Your Way In

    Getting drugs of any sort through the blood-brain barrier is never something that can be taken for granted, and if your therapeutic agents is well outside the usual size/polarity bounds, you can pretty much take it for granted that it’s not going in at all. The number of techniques that have been tried to get… Read More
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