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  • 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
  • The Scientific Literature

    The EU Open Access Fight Continues

    I wrote here about a European plan to mandate open-access scientific publication – one whose sweep many found startling when it was proposed. And some of the ones who were startled were researchers themselves, it seems – here’s an open letter opposing the plan as written. Chemists seem to be among those leading the charge… Read More
  • Biological News

    Engineering Biology, For Real?

    Any article titled “How to Engineer Biology” is going to get a look from me – and when I’m referenced in the opening paragraphs, especially so. This is a piece by Vijay Pande in Scientific American, and I get called out for my naming of the “Andy Grove Fallacy” (found in this post and the… Read More
  • Who Discovers and Why

    A Difficult Birth For Some Ideas

    This fascinating article has nothing to do with drug discovery per se, but it has plenty to do with discovery itself. It’s a memoir of the author’s physicist grandfather, who believed while working at his job at Oak Ridge that he might have come across a big result in probability as related to quantum mechanics… Read More
  • Chemical News

    Here’s What’s Been Done Before

    I enjoyed this ACS Med. Chem. Letters perspective on AI and machine learning in medicinal chemistry. It has several good points to make, and it brought up one that I haven’t gone into here before: if you’re mining the literature, you will get what the literature can tell you. At the very best, the high… 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
  • General Scientific News

    Hail to the Ribbon

    A correspondent sent along this item, celebrating the inventor of something that’s so ubiquitous in molecular biology and protein chemistry that you have to think for a moment to realize that it had an inventor: the ribbon diagram. That’s Jane Richardson of Duke, who started there in 1969, back when there were only about 20… Read More
  • Biological News

    Real Progress in Parkinson’s

    There have been some potentially significant developments in Parkinson’s disease, which is a good thing to be able to report. As populations age around the world, PD has been on its way up, but therapies for it have not been, despite a good deal of work in the field. But it looks like some clues… 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
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