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Posts tagged with "Pharmacokinetics"

  • Cancer

    Vitamin C and Immuno-oncology

    Linus Pauling was a fearsomely great scientist who is remembered by the general public for his advocacy of megadoses of Vitamin C, a favorite topic of his later in life. Infectious disease, cancer: Pauling advised gram amounts of ascorbic acid and had a lot of theorizing to offer about why that was beneficial. So while… Read More
  • Clinical Trials

    Idiosyncratic Tox

    It’s our high failure rate in clinical trials that makes the drug industry what it is. And two of the biggest factors in that failure rate are picking the wrong targets/mechanisms, and unexpected toxicity. The first is clearly a failure of our understanding of human biology, and the only remedy I can see for that… Read More
  • Alzheimer's Disease

    Congo Red

    Many roots of organic chemistry, and of medicinal chemistry in particular, often originate in what might seem like an unlikely place: the dyestuff industry of the late 19th century. I had already known this to some degree, but writing the historical vignettes in The Chemistry Book really brought it home to me. And if you… Read More
  • Chemical Biology

    Membrane Surprises

    Drug discovery folks spend a good amount of time and effort dealing with cell membranes. Our drug candidates stick to them, get imbedded in them, might have to slip through them to get to their target proteins, or may target proteins that are localized in them, can get actively transported through them or actively pumped… Read More
  • Clinical Trials

    Drug Dosing

    First in humans! That’s a big step for a drug project – you’ve identified a clinical candidate with enough potency, selectivity, etc. to be a plausible drug, you’ve made it past toxicity testing (always a black-box cross-your-fingers exercise), and you’ve figured out a way to dose the stuff in human subjects. But how d… Read More
  • 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
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