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Posts tagged with "Drug Development"

  • 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
  • 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

    A Nobel for Immuno-Oncology

    As many had expected, the Nobel prize in medicine/physiology this year recognizes advances in immuno-oncology: James Allison (for CTLA4) and Tasuku Honjo (PD-1). For some years now, that has been a huge, massive, unstoppable wave in cancer research, and I would not want to try to estimate how much time, effort, and money has gone… 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
  • Clinical Trials

    Digging Into the Genetics of Drug Targets

    Rare diseases – remember years ago, back when those were a case of market failure? When companies were reluctant to work on them because the market size was guaranteed to be small and you’d have to charge, like, a hundred thousand or more a year to make the whole idea financially viable? Which wasn’t going… Read More
  • Business and Markets

    Anarchist Drugs For All. Yeahboy.

    I’ve had numerous requests for my opinion about this article, so here it comes: it’s largely bullshit. It’s about “a volunteer network of anarchists and hackers developing DIY medical technologies”, and I can see why Vice.com is running the article, because that drugs/anarchists/hackers combo is absolute catnip to thei… Read More
  • Drug Development

    On Jadedness

    It’s a Friday in midsummer, so I assume that a fair percentage of the readership is not even around! So I’m not going to do a huge detailed blog post (got one of those coming on Monday, actually). Today I just wanted to go on a bit about a problem that comes with experience in… Read More
  • Alzheimer's Disease

    The Case of Verge Genomics

    A number of people have passed along the recent press stories about Verge Genomics, a new company out of YCombinator that has just raised $32 million for neuroscience drug discovery. Now that, as literally anyone who’s ever done it can tell you, is a hard field of a hard field, and I wish Verge good… Read More
  • Analytical Chemistry

    The Entropic Term is Laughing At Us

    There are plenty of things to optimize in a med-chem project other than binding affinity. But if you don’t have at least some level of binding, you may not have a med-chem project. And while from the outside, you might think that understanding how and why compound A binds to a given target while compound… Read More
  • Cancer

    Why Not Target DNA? Well. . .

    There are all sorts of small-molecule drugs that bind to protein targets. Active sites of enzymes are, of course, a big subset of those, but there are plenty of enzymes whose allosteric sites are known to host synthetic ligands as well. Membrane receptor and ion channel proteins get both of those mechanisms too, and then… Read More
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