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Posts tagged with "Pharmacokinetics"

  • Chemical News

    Saturated Heterocyclic Rings And Their Personalities

    Here’s a ring system that you’ve never used before – the cyclopropyl system in purple at the end of the row in the diagram at right. It’s described in this paper from GSK-Stevenage as a new morpholine isostere. A 4-morpholino-pyrimidine hinge binder core is preferred in many PI3K and PIKK inhibitors, but the team was… Read More
  • Biological News

    Nanobodies Get Their Due

    Hot new technologies! We have waves of them in this business, and everyone talks about them, spends money looking at them, and does deals with small companies who are formed around them. But then reality sets in: only a few of these things march forward into the clinic, and even fewer emerge on the other… Read More
  • Pharmacokinetics

    Gut Bacteria, Pitching In

    When a patient takes an oral dose of a drug, you can picture it as being a little like one of the those Japanese pachinko machines, where a ball drops into a maze of complicated bouncing paths on its way to the bottom. There are a lot of things that happen once a pill hits… Read More
  • Pharmacokinetics

    There Is No “Depression Gene”

    I wrote a couple of years ago about the long-running study of mutations in a serotonin transporter gene. Over the years, polymorphism in the gene have been correlated with all sorts of human behavior and psychiatry, in keeping with the importance of serotonin signaling in human cognition. Depression, anxiety, that whole end of human behavior… 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
  • 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
  • Animal Testing

    A Toxicological Flag

        Here’s a caution from a new paper out of Manchester. The group had been synthesizing inhibitors of PARG (poly-ADP ribose glycohydrolase), an enzyme involved in DNA repair. The general chemotype is shown at right, but there are a number of variations. That fluorine is a new addition, though. The corresponding cyclopropylmethyl se… Read More
  • Cancer

    Replacing Antibodies With Small Molecules

    As anyone who’s been following the oncology field knows, antibodies against either the PD-1 receptor or its ligand PD-L1 are about the biggest things going in the field right now. Hundreds of clinical trials are underway against various tumor types and in various combinations, in the effort to see how far the immuno-oncology idea can… Read More
  • Biological News

    Sunlight And the Brain

    One of the impressive things about biochemistry and cell biology is how it can produce physical correlates to things that we know and experience, but have no detailed explanation for. There’s a really interesting example out in Cell that has to do with the effects of sunlight on mood and learning. Those effects are real, but… Read More
  • Chemical News

    Simple Rings, Simply Wrong

    Medicinal chemists spend a lot of time thinking about the relative greasiness of their molecules. Being professional scientists, of course, we have come up with some slightly more quantitative phrases than “relative greasiness”, but that’s definitely the idea. How hydrophilic/hydrophobic a compound is determines not to what extent… Read More
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