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  • Chemical News

    Stop Ignoring the Sugars!

    This paper (from two groups at Yale’s chemistry department) addresses several important things that fall into the “important irritants” category in synthesis and molecular biology – or maybe that should be “irritatingly important”. We spend a lot of time thinking about proteins in terms of their primary sequence… Read More
  • Alzheimer's Disease

    Merck’s BACE-Inhibitor Alzheimer’s Wipeout

    I mentioned last year that Merck’s BACE inhibitor trial for Alzheimer’s had been stopped for futility. Now here’s the full writeup in NEJM, and futility appears to have been le mot juste. There were two treatment groups (12 mg and 40 mg), and in neither one did the ADAS-cog or ADAS-ADL scores (scales for degree… Read More
  • Drug Assays

    Pharmacokinetic Advice From Genentech

    Here’s another solid pharmacokinetics paper, this one from Genentech, with advice on how to extend drug half-life (compare this other recent one). They’re specifically addressing the “make it less lipophilic” rule of thumb that many medicinal chemists have, and they demonstrate that this isn’t exactly a universal law.… Read More
  • Cancer

    Cancer Sequencing Hype And Reality

    This piece in Science says something that needs to be said louder and more publicly. If you live in the US, you’ve surely seen various cancer treatment centers talking about their personalized therapy plans, and especially how they’ll tailor things to your DNA sequence and so on. You would get the impression that we have… Read More
  • Cancer

    IDO Appears to Have Wiped Out

    We have the answer to a question posed here earlier this month. That was after the Merck/Incyte failure of a combination of Keytruda and Incyte’s IDO (indole 2,3-dioxygenase) inhibitor. That mechanism was supposed to increase T-cell activity, but the trial showed it to have no effect on Keytruda’s efficacy at all. Earlier IDO trials had… Read More
  • Drug Assays

    Tecfidera Explained

    One of the more unusual drugs on the market is Tecfidera (dimethyl fumarate). I went into its history a bit in this post, if you’re wondering how a molecule that small and unfunctionalized became a multiple sclerosis drug. As that shows, it went into trials for the disease with quite a bit of clinical rationale… Read More
  • Chemical Biology

    4-Azidophenylalanine: A Warning

    There’s a reagent used in chemical biology and protein labeling that should be getting a bit more attention than it does. Not because it’s useful – that’s already known – but because it can explode. Here’s the paper (from UC-Irvine and Amgen), and the compound is the 4-azido derivative of phenylalanine. Interest… Read More
  • Drug Assays

    DNA Libraries Are Here to Stay

    Here’s an update from Alex Satz of Roche on DNA-encoded library (DEL) screening. I’ve been mentioning this technique on the blog since its early days, and I freely admit that when it was starting out I had trouble believing that it worked (or even could work). The idea, in short, is that you  append a… Read More
  • Chemical News

    Calculate Your Way Out of Bad Yields

    I wrote a little while back about a brute-force approach to finding metal-catalyzed coupling conditions. These reactions have a lot of variables in them and can be notoriously finicky about what combination of these will actually give decent amounts of product. At the same time, it appears that almost any given metal-catalyzed coupling reaction is… Read More
  • Biological News

    The Fuzzy Free-For-All

    I wrote here about the way that disordered proteins seem to be able to bind together tightly in the apparent absence of a defined structure, and along the way I expressed a desire not to lead any drug discovery efforts against such systems. Now here’s another example of protein fuzziness, and I can’t say that… Read More
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