Skip to main content
Menu

Posts tagged with "Pharmacokinetics"

  • Chemical Biology

    Inside the Lipid Droplets

    Figuring out an unusual natural product’s activity can be a difficult but rewarding exercise. Deep evolutionary time has provided us with a bizarre range of chemical structures that are presumably not being synthesized by organisms for the sheer fun of it – these things are acting as signaling molecules, antifeedants, poisons for the co… Read More
  • Analytical Chemistry

    March of the Raman Images

    Well, since I mentioned just the other day (and not for the first time) that determining drug concentrations and localization in cells is a major unsolved problem, I should probably talk about this new paper (a collaboration between groups in Edinburgh and Glasgow, nice to see since their cities are not always collaborative in all… Read More
  • Diabetes and Obesity

    Proteins as Oral Drugs: Possible, But Not Probable

    I have been writing this blog for some time (!) That occurs to me on seeing this article in Nature Reviews Drug Discovery on oral dosing of peptide drugs – I say that because of this 2002 post on the very same subject, at the time directed towards the then-still-somewhat-hot topic of Judah Folkman’s endostatin angiogenesis… Read More
  • Pharmacokinetics

    Drugs Inside Cells: How Hard Can It Be, Right?

    One would imagine that we drug discovery and development types have a reasonable handle on how much of our latest candidate compound makes it into cells. And that we would further know how much of that is floating around freely in there, versus tied up to some protein or another. One could not be more… Read More
  • 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
123...