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Posts tagged with "Drug Assays"

  • Analytical Chemistry

    The Infinitely Active Impurity

    Yesterday’s post touched on something that all experienced drug discovery people have been through: the compound that works – until a new batch is made. Then it doesn’t work so well. What to do? You have a fork in the road here: one route is labeled “Blame the Assay” and the other one is “Blame… Read More
  • Aging and Lifespan

    GSK and Sirtris: A Bit More

    Nature has a short item on the Pfizer paper that questions the reproducibility of some key sirtuin work (covered here and here). There are some good points to temper the pessimism. Leonard Guarente of MIT, a key pioneer in the field, says: “. . . that the latest findings are neither surprising nor worrisome. The… Read More
  • Aging and Lifespan

    The Sirtris Compounds: Worthless? Really?

    As followers of the drug industry know, GlaxoSmithKline famously paid $720 million to buy Sirtris Pharmaceuticals in 2008. Sirtris is the most high-profile shop working on sirtuins and resveratrol-like pharmacology, which subject has received a massive amount of press (some accurate, some scrambled). I’ve been following the story with interes… Read More
  • Analytical Chemistry

    Run It Past the Chemists

    I missed this paper when it came out back in October: “Reactome Array: Forging a Link Between Metabolome and Genome“. I’d like to imagine that it was the ome-heavy title itself that drove me away, but I have to admit that I would have looked it over had I noticed it. And I probably should… Read More
  • Drug Assays

    Selective Scaffolds

    We spend a lot of time in this business talking about molecular scaffolds – separate chemical cores that we elaborate into more advanced compounds. And there’s no doubt that such things exist, but is part of the reason they exist just an outcome of the way chemical research is done? Some analysis in the past… Read More
  • Drug Assays

    Why Don’t We Have More Protein-Protein Drug Molecules?

    Almost all of the drugs on the market target one or more small-molecule binding sites on proteins. But there’s a lot more to the world than small-molecule binding sites. Proteins spend a vast amount of time interacting with other proteins, in vital ways that we’d like to be able to affect. But those binding events… Read More
  • Analytical Chemistry

    More Binding Site Weirdness

    Now here’s an oddity: medicinal chemists are used to seeing the two enantiomers (mirror image compounds, for those outside the field) showing different activity. After all, proteins are chiral, and can recognize such things – in fact, it’s a bit worrisome when the enantiomers don’t show different profiles against a protein t… Read More
  • Drug Assays

    Side Effects, Predicted?

    There’s a new paper out in Nature that presents an intriguing way to look for off-target effects of drug candidates. The authors (a large multi-center team) looked at a large number of known drugs (or well-characterized clinical candidates) and their activity profiles. They then characterized the protein targets by the similarities of the mol… Read More
  • Drug Assays

    Lumpy Assay Results

    When we screen zillions of compounds from our files against a new drug target, what can we expect? How many hits will we get, and what percentage of those are actually worth looking at in more detail? These are long-running questions, but over the last twenty years some lessons have been learned. A new paper… Read More
  • Aging and Lifespan

    What Exactly Does Resveratrol Do?

    Resveratrol’s a mighty interesting compound. It seems to extend lifespan in yeast and various lower organisms, and has a wide range of effects in mice. Famously, GlaxoSmithKline has expensively bought out Sirtris, a company whose entire research program started with resveratrol and similar compound that modulate the SIRT1 pathway. But does it… Read More
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