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Posts tagged with "Drug Assays"

  • Cancer

    Bromopyruvate Revealed

    3-bromopyruvate is an interesting and controversial compound. It’s been reported to be an active chemotherapy agent, apparently acting via covalent inhibition of glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and subsequent metabolic effects via loss of pyruvate itself. Several years ago, you could come across numerous web pages touting it… Read More
  • Drug Assays

    A Magic Methyl, Spotted in the Wild

    You hear medicinal chemists talking about the “magic methyl”, the big effect that a single CH3 group can have on potency or selectivity. Here’s a new J. Med. Chem. paper that shows one in action.That structure looks like a kinase inhibitor if anything ever did, and so it is. But small changes to it can… Read More
  • Analytical Chemistry

    That One Serotonin Receptor

    Serotonin is perhaps the only neurotransmitter molecule that you could find named in a random poll, thanks to its association with antidepressants. (That association is far messier than popular opinion realizes, but that’s another topic). It’s a complicated one to have embraced, that’s for sure. There are 13 subtypes of GPCR serot… Read More
  • Drug Assays

    Ligand Efficiency Rethought

    Peter Kenny has a paper out on ligand efficiency that’s required reading for medicinal chemists using (or thinking about) that concept as a design tool. I’d recommend reading it with this recent paper – between the two of them, you’re going to have references to a huge swath of the literature on how to measure… Read More
  • Cancer

    Drug Repurposing, Computed

    Here’s an example of something that we’re all going to see more of in the coming years: the computational approach to biochemical pathway discovery and (potentially) new therapies. In this case, the authors are looking at some pretty intractable tumor types (type 3 and type 4 medulloblastoma), which is a good place for discovery in… Read More
  • Chemical News

    CDK Inhibitors: Purchase With Caution

    Cyclin-dependent kinase (CDKs) have been drug targets for quite a while now. There are 20 different ones, and they help to regulate a whole list of important functions, particularly involving the cell cycle (which has made them of great interest in oncology research). There are three approved drugs in the area so far: Kisqali (ribociclib)… Read More
  • Analytical Chemistry

    Knowing the Structure

    There are a lot of topics that we really should know more about in drug discovery, but which are buried inside projects inside particular organizations. Some of this knowledge is available once you’re inside said organization, but some of it is hard to assemble even then (much less into a review from outside). An example… Read More
  • Biological News

    The Chemistry Nobels, 2018

    The 2018 Nobel Prize in Chemistry has gone to Frances Arnold (for directed evolution of enzymes) and to George Smith and Gregory Winter for phage display. These are worthy discoveries, techniques that have gone on to be used for a huge variety of work ranging from blue-sky research to marketed drugs, and the Nobel committee… Read More
  • Drug Assays

    A New Antibiotic? Yes, Please

    New antibiotics against resistant Gram-negative bacteria make me happy, so I’m very glad to see this report from Genentech. They’ve been doing a lot of work on an antibiotic scaffold (arylomycins, Update: on a program that came in whey they bought RQx) which had not thus far really found much practical use, and it looks… Read More
  • Drug Assays

    Virtual Compound Screening: The State of the Art

    Here’s an interesting article from a former colleague of mine, Pat Walters, on virtual chemical libraries. Those, of course, are meant to fill in the (large, enormous, humungous) gap between “compounds that we have on hand to screen” and “compounds that we could screen if we actually had them”. That second group, if ta… Read More
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