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  • Alzheimer's Disease

    A Brief Note About Alzheimer’s

    Well, there it is. Biogen and Eisai have announced just this morning that they’re halting Phase III trials of aducanumab, their anti-amyloid antibody, after the monitoring committee judged that further treatment would be futile. I’m not going to do some sort of victory dance, because (once again) this is bad news for Alzheimer’s… Read More
  • Cancer

    An Unexpected Halt in Multiple Myeloma for Venetoclax

      Venetoclax (ABT-199) is an unusual drug. But now there’s some unusually bad (and unexpected) news about it. That’s the structure at right, and medicinal chemists will understand immediately why it’s a bit of an outlier. With a molecular weight of 868, that structure just keeps on going, with a somefeatures that you donR… Read More
  • Chemical News

    New Chemistry, Making New Things

    In a perverse way, I’m enjoying how modern organic synthesis is upsetting the classic undergraduate sort of test-question syntheses. You know – Grignards, ester condensations, oxidation and reduction of carbonyls, Wittigs, Sandmeyer reactions, Friedel-Crafts, good ol’ hammer-and-tongs bond formation. I had sophomore organic back i… Read More
  • Business and Markets

    Drug Industry Consolidation Refuses To Arrive So Quickly

    Anyone who’s watched the biopharmaceutical landscape over the years is familiar with two large forces that reshape the list of companies in the area: on one end, you have mergers and acquisitions that decrease the number of firms, and on the other you have startups that increase it. How have these two been balancing out?… Read More
  • Business and Markets

    Zafgen: Will There Be a Third Act?

    A few years ago on this blog, I wrote several times about a small company called Zafgen and their unusual epoxide-based chemical matter (beloranib) that was in development for the rare Prader-Willi syndrome. That’s a genetic disorder that includes, among many other problems, constant hunger (with the complications that you’d expect fro… Read More
  • Chemical Biology

    Sneaking Proteins Into Cells

    Now here’s a weird and rather startling paper. One of the things that people in this line of work spend a lot of time on is getting things into living cells. Small molecules often slide in, one way or another (although, to be honest, our detailed understanding of how they do that could use some… Read More
  • Chemical Biology

    What Those Degraders Are Actually Doing

    Since targeted protein degradation is such a hot topic these days, this paper (which adds to the results obtained by this one) should get some interest. It’s a report of a detailed look at the kinetic behavior of several bifunctional degraders – and there’s a lot of kinetic behavior to look at. That’s because you’re l… Read More
  • Drug Assays

    Experiences With Phenotypic Screening?

    Very little blogging time today, but I wanted to throw a question out to the readership instead. I’m at the Keystone conference on Phenotypic Drug Discovery, so here’s a relevant topic: what are your own experiences with phenotypic screening? Background for those outside the field: broadly speaking, you can sneak up on a drug by… Read More
  • Regulatory Affairs

    A New FDA Commissioner, Suddenly

    The big news late yesterday afternoon was the resignation of Scott Gottlieb as FDA commissioner. I have no idea why he’s leaving, naturally. He’s spoken about wanting to spend more time with his family and being dissatisfied with going back and forth between Connecticut and DC, and I have no doubt that both of those… Read More
  • Chemical Biology

    More Fragment Binding In Cells – Now With Less Confusion

    The Cravatt group (in collaboration with partners from Harvard and Bristol-Myers Squibb) has a paper out on Chemrxiv that’s a followup to a 2017 paper of theirs which (I will freely admit) is one of my favorites. That was on taking fragment-sized compounds (and a slightly higher-MW collection), each labeled with a diazirene (for photoaffinity… Read More
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