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Posts tagged with "Drug Assays"

  • Animal Testing

    Mutated Mutations (And Other Rodent Study Problems)

    Here’s one for the “Dang it, now I have to think about that, too” file. A recent paper suggests that there are mutations in many genetically modified mouse models that could well be confounding their phenotypes. The problem is that so many of these are done from very similar embryonic stem cells and in very… Read More
  • Biological News

    Target Invalidation

    Target validation is a key process in drug discovery, naturally. But it’s worth remembering that target invalidation happens more often, and is also important. The first project I worked on in the drug industry proved pretty conclusively that selective antagonism at the D1 dopamine receptor is not an effective therapy for schizophrenia, des… Read More
  • Diabetes and Obesity

    Zebrafish, Finally Taking Over as Foretold

    The idea of phenotypic screening is not new, but once you bring up the topic, you find that different people have different ideas about what a phenotypic screen really is. As has been discussed around here before, not everyone buys into the concept of a cell-based screen as “phenotypic”, but I’m willing to believe in the… Read More
  • Biological News

    Chemical Probe Compounds: Time to Get Real

    Update: the chemical probes portal mentioned here has since been updated and re-launched. There’s a new paper on chemical probes out in Nature Chemical Biology, and right off, I have to disclose a conflict of interest. I’m a co-author, and I’m glad to be one. (Here’s a comment at Nature News, and here’s one at… Read More
  • Chemical Biology

    Lipids, Proteins, and Chapman’s Homer

    Longtime readers might recall that every so often I hit on the topic of the “dark matter” of drug target space. We have a lot of agents that hit G-protein coupled receptor proteins, and plenty that inhibit enzymes. Those, though, are all small-molecule binding sites, optimized by evolution to hold on to molecules roughly the… Read More
  • Alzheimer's Disease

    Two Alzheimer’s Updates (Lilly and TauRx)

    When you look at the stock charts of the major pharma companies, there’s not a lot of excitement to be had. Until you get to Eli Lilly, that is. Over the last year, the S&P 500 is up about 5%, and most of the big drug stocks are actually negative (Merck -0.4%, Sanofi down 6%… Read More
  • Drug Assays

    A Look at Phenotypic Screening

    Here’s a good overview of phenotypic screening from a group at Pfizer in Science Translational Medicine. It emphasizes, as it should, that this is very much a “measure twice, cut once” field – a bad phenotypic screen is the worst of both worlds: The karyotype of a cell represents one of its most fundamental and… Read More
  • Drug Assays

    The End of Compound Property Optimization Is At Hand

    Here’s another Big Retrospective Review of drug pipeline attrition. This sort of effort goes back to the now-famous Rule-of-Five work, and readers will recall the Pfizer roundup of a few years back, followed by an AstraZeneca one (which didn’t always recapitulate the Pfizer pfindings, either). This latest is a joint effort to look at th… Read More
  • Animal Testing

    Organ Models on Chips

    Why do we test new drug candidates on animals? The simple answer is that there’s nothing else like an animal. There are clearly chemical and biological features of living systems that we don’t yet understand, or even realize exist – the discovery of things like siRNAs is enough proof of that. So you’re not going… Read More
  • Drug Assays

    Target (In)validation

    Here’s a short review in ACS Medicinal Chemistry Letters on target validation. As the author (Ramzi Sweis of AbbVie) says, it’s easy for medicinal chemists to lose track of that being part of their role: Too often, medicinal chemistry teams blindly accept the biological underpinnings of a new program as sound and are unaware that… Read More
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