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Posts tagged with "Cancer"

  • Cancer

    Your Cancer Targets May Not Be Real

    I wrote here about a paper from Cold Spring Harbor labs that invalidated MELK as a cancer target. That was straightforward enough: knocking it out via CRISPR across a whole range of cancer cell lines had no effect on their growth at all, so it’s kind of hard to make the case that it’s an… Read More
  • Business and Markets

    The Last of Stemcentrx

    The final implosion of the Stemcentrx deal is worth a note, although I said a lot of what I have to say about it back in December. I want to especially emphasize two points I made back then – first, that the failure of this whole acquisition is different only in degree, and not in… Read More
  • Biological News

    Unfolding the Unfolded Protein Response.

    When you look closely at cellular biochemistry, what you see are a lot of amazing processes that are surrounded by amazing amounts of redundancy, backups, patches, and accumulated tweaks and fixes. That’s evolution for you; these things have been piling up for a billion years or two, and we’re all the descendants of the critters… Read More
  • Biological News

    Slow Down That Protein’s Travel Plans

    Here’s a new look at the various ways that small molecules can affect a well-known drug target (the estrogen receptor) and it shows us that we’re all going to have to look at these things more carefully than we do. Now, to be fair, the ER is already fairly complicated, because it’s a nuclear receptor. Read More
  • Cancer

    The Most Synthetically Complex Drug Candidate Ever

    This is quite a synthetic chemistry accomplishment: the halichondrin derivative E7130 has been synthesized on an 11-gram scale by the Kishi group (open-access paper). I’ve copied that structure directly from the published paper, because there’s just not enough time this morning to redraw it! This would surely be the most complex natural… Read More
  • Cancer

    Making and Measuring Multivalency

    Here’s an unusual paper that’s studying receptor behavior on cell surfaces by use of atomic force microscopy. (Here’s the SI file, which is free to access). The authors took the marketed VEGF inhibitor vandetanib (VD6474) and attached it through linkers to the AFM tip, and then scanned around the surface of live human umbilical v… Read More
  • Business and Markets

    Sorrento Therapeutics Is Not Happy

    I have not been a fan of Patrick Soon-Shiong and his approach to the biopharma business (and the publicity thereof). There’s a new lawsuit that (should its accusation hold up) will make anyone even less of a fan. Here’s a rundown at Endpoints, and one at Forbes. It’s a mess, so I’ll try to untangle… Read More
  • Cancer

    No Pain, and No Worries?

    The FAAH (fatty acid amide hydrolase) enzyme system has provided a number of headlines over the years. FAAH itself is involved in the brain’s endocannabinoid system – it clears neurotransmitters like anandamide – and a number of other biologically important hydroxyethylamide and acyltaurines. So the potential for inhibitors of it… 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
  • "Me Too" Drugs

    Proteasome Inhibitors, Refined

    The proteasome is quite the structure. It is the shredding unit of the cell, where no-longer-needed proteins go to be ripped down to their components for recycling, and it’s become a more and more important part of drug discovery over the years. For one thing, all this fashionable targeted protein degradation work is about sending… Read More
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