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Posts tagged with "Toxicology"

  • 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
  • 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
  • "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
  • Business and Markets

    The Clinic Giveth And Most Definitely Taketh Away

    There have been some pretty dramatic clinical trial results coming out recently, and unfortunately drama is a variable that can take either a positive or a negative sign in front of it. On the plus side, MacroGenix, a company that not many people had been paying attention to, announced results of a head-to-head trial of… 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
  • Analytical Chemistry

    The Sartan Contamination Story

    There’s a chemical contamination story in the generic drug industry that just isn’t going away. Late last summer, some lots of valsartan were recalled due to detection of N-nitrosodimethylamine (NDMA), and the problem has just continued since then. We’ll get into the chemistry of this problem in a minute, but first off, looking at… Read More
  • Cancer

    Bromopyruvate Revealed

    3-bromopyruvate is an interesting and controversial compound. It’s been reported to be an active chemotherapy agent, apparently acting via covalent inhibition of glyceraldehyde 3-phosphate dehydrogenase (GAPDH) and subsequent metabolic effects via loss of pyruvate itself. Several years ago, you could come across numerous web pages touting it… Read More
  • Biological News

    Real Progress in Parkinson’s

    There have been some potentially significant developments in Parkinson’s disease, which is a good thing to be able to report. As populations age around the world, PD has been on its way up, but therapies for it have not been, despite a good deal of work in the field. But it looks like some clues… Read More
  • Clinical Trials

    Digging Into the Genetics of Drug Targets

    Rare diseases – remember years ago, back when those were a case of market failure? When companies were reluctant to work on them because the market size was guaranteed to be small and you’d have to charge, like, a hundred thousand or more a year to make the whole idea financially viable? Which wasn’t going… Read More
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