1/16/2019

953-956 days to go – 31 months

Biopharma/Investing
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Not surprised APTX doesn’t work. The depression stuff doesn’t work either.

Papers I’ve Read
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Discovery and characterization of AZD6738, a potent inhibitor of ataxia telangiectasia mutated and rad3 related (ATR) kinase with application as an anti-cancer agent. Foote et al. J Med Chem 2018.
AstraZeneca’s ATR project has yielded a clinical candidate. 6738 is a suloximine (S=N), replacing the sulfonamide moiety of the hit AZ20. Apparently, this SNOH- moiety hanging off the cyclopropyl did the trick to improve solubility and eliminate CYP3A4 liability (that and one atom on the heterocycle). Anyway, ATR is part of DNA damage repair. You’ve probably heard of it from Vertex, who sold their VX-970 to Merck KgaA (now M-6620 or berzosertib) for a pretty penny. I don’t trust anything from Vertex Cambridge drug discovery (including and especially Derek Lowe). So far I don’t think anyone is bowled over by the data for ATRs–no monotherapy efficacy. There’s a Bayer compound out there, too. It seems like the AZ predecessor compound was around for a while.

6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB1) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity. Zhang et al. J Med Chem 2018.
J&J researchers produce a peripherally-restricted CB1 agonist to avoid the AE profile of the storied Accomplia. I didn’t know GC1 was the MOST abundant GPCR in the brain–kind of amazing, huh?

Cytokine-Induced Expression of HIV-1 in a Chronically Infected Promonocyte Cell Line. Folks, Fauci, et al. Science 1987.
Human Immunodeficiency Virus-Infected Individuals Contain Provirus in Small Numbers of Perpiheral Mononuclear Cells and at Low Copy Numbers. Simmonds, et al. J Virol 1990.

Still in the way-back-machine for HIV.

Personal
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Lauren Duca divorced her husband and is gay now. Just 2 and a half years ago she thought it was wise to marry a man. Now all she tweets about is how terrible and useless men are. Play to your audience, I guess. Perhaps she will even become an author, selling her book to a like-minded left-wing gnat (or nut?) at a publishing company that doesn’t realize they’ve been appropriated by ideology. Maybe I should rollup that industry and instill some libertarianism. People should be able to read whatever is appealing, not what some self-anointed anti-business SJW gatekeeper decides.

I wrote more on this and recent revelations that Duca is a body-shamer (the body-shaming posts are awful) and even an ablist/classist as she panned community colleges in a recent Facebook post if you’d like to read it. Evidently even further revelations are forthcoming. Guess her book deal may be off-the-table.

16 thoughts on “1/16/2019”

  1. These posts show me that Martin A) has a serious work ethic, B) cares about his work and C) isn’t gonna be fucked over by politics

  2. I’m not really a Duca fan ( Dookie) we call her. L o l.
    I don’t know know how she may ever possibly had been new . This story shame story on men she pulled is symptomatic insanity
    By the way , her stockings are always lovely.💘

  3. She likely went full girl love because you showed interest in her… Thinking out loud, here. Why do you even care what she does? I AM YOUR WIFE! 😂🤣 I was not aware you could peruse FB while in prison. You are legit a stalker. No worries. To know a stalker is to love a stalker. 🤓

  4. Shkreli, you have to reply to some of the comments people post or really what’s the point in having a comment section? In so many ways you are dumb…. Thank God there are real geniuses out here paying attention.

  5. Hang in there Shkreli. We’re all rooting for you. I’ll also be highly disappointed if you don’t get right back in the pharma game the second you’re released.

  6. Really was enjoying your youtube videos. Excited for you to get released. Physical laws haven’t changed much since you’ve been incarcerated, so you haven’t missed a great deal, but it’s still very sad that you have to spend any time at all in prison.

    #freeMartinShkreli

  7. Become impatient or angry when they don’t receive special treatment

    React with rage or contempt and try to belittle the other person to make themselves appear superior

  8. Whenever I hear Lauren Duca mentioned I get an image of Martin, doing a Cartman impression, screaming that he is going to F**k her. I’d never heard of her before he made her his Nemesis.

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