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Posts tagged with "Drug Assays"

  • Animal Testing

    Melanocortin: It’s Not Just For Lizards Any More

    If you’re looking for a good example of evolution-as-a-tinkerer, the melanocortin receptors would be a good place to start. From a single starting point, they’ve ended up as a family of related proteins that do completely different things. And the hormones that bind to them have radiated out as well: they’re all derived by process… Read More
  • Chemical Biology

    HAT Inhibitors: Interpret With Care

    There are quite a few histone deacetylase inhibitors out there, from research tools to FDA-approved drugs. Those inhibit the enzymes that remove the acetyl epigenetic markers from histone proteins – but what about inhibitors of the enzymes that put them on? Those are histone acetyltransferases (HATs), and they’ve naturally been the subj… Read More
  • Chemical Biology

    Poke Holes Through Your Membranes. It’s Fun.

    The cell membrane – the fundamental architecture of living things, the foundation of how our very bodies are organized – is a major pain in the behind. I express this ungrateful opinion merely because over the years it has rejected entry to some of my best ideas for drug candidates, and I bear a grudge. Read More
  • Chemical News

    How Many of Those Compounds Are Crap?

    A reader sent along a note about this letter to Nature Medicine earlier in the year. It’s about drug repurposing, and more specifically about the Drug Repurposing Hub at the Broad Institute. This is a collection of nearly 5,000 compounds, curated and annotated with their histories and activities. It was not a straightforward task: . Read More
  • Cancer

    There Are Probes, And There Are Probes

    A friend in the business called my attention to this paper, which is about another piece of the ubiquitination system that I was writing about here just the other day – in this case, the deubiquitinating enzyme Rpn11. There are a couple of classes of deubiquitinators – some of them use a cysteine in their… Read More
  • Drug Assays

    Beware of Zinc. And of Other Stuff.

    Here’s a paper that will give many medicinal chemists a shiver of recognition. A group from Dundee reports a screening hit against the enzyme Ube2T, a ubiquitin-conjugating (E2) enzyme. For those outside the field, ubiquitin is indeed ubiquitous. It’s a short bit of protein that gets hung onto other proteins (or removed, if it’s t… Read More
  • Drug Assays

    Whole Classes of Things

    We all know about target-based drug discovery. Enough biology has been learned that we think that Protein X is operating at a crucial stage in the development of Disease A, so we’re going to try to find an inhibitor/agonist/antagonist, a ligand/allosteric modulator/binder/potentiator, or something to somehow affect its actions. We’ve se… Read More
  • Biological News

    Those Compounds Aren’t What You Think They Are

    There’s a lot of work in the literature on the TrkB receptor, which responds to brain-derived neutrotrophic factor (BDNF). That name certainly makes the ligand protein sound like a pretty big deal, and so it is: BDNF is involved in a lot of neural development pathways, injuries to nerve tissue, and the like, and given… Read More
  • Chemical Biology

    A Tour of the Outer Precincts

    You know, in an odd way, I’m actually more optimistic about drug discovery than I was a few years back. It’s due to the new tools that we have in molecular and cellular biology that we didn’t have before, and it’s also the number of unusual and interesting approaches that are being taken on the… Read More
  • Drug Assays

    Phenotypic Screening: The State of the Art

    I can recommend this article on phenotypic drug discovery from the latest Nature Reviews Drug Discovery. (For the nonspecialists in the crowd, there are two broad categories of screening for drug leads. One is “target-directed”, where you have an idea from other studies about what protein or pathway you want to affect, and you set… Read More
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