Monday, December 3, 2007

There’s a controversy about AIDS drugs?




There’s a controversy about AIDS drugs?

While we wait for Dr. James J. La Clair to get around to answering those questions below (not… holding… breath…) (nevermind, he’s still here) let’s move on with the bloggotronix and hit up the lately azt.gifforgotten Drug Sunday! In keeping with the theme of controversies, I found an interesting one with the modern plague, HIV. The combination of the extraordinary immaturity of the two initial discoverers of the HIV virus, Robert Gallo and Luc Montagnier and the absurd claims of formerly respected cellular biologist Peter Duesberg, have created a science melodrama which one could easily fall in love with. According to Duesberg, HIV is the net result of being gay and doing amyl nitrites to loosen up your pooper, doing methamphetamines and then a few nostrils full of cocaine and finally the damn AZT you take because you get sick from all your gayness and drugs. In a nutshell, if you would just STOP BEING GAY DRUG ADDICTS YOUR AIDS WOULD GO AWAY. Naturally Peter Duesberg took a lot of shit for this. All this got me thinking about a drug Duesberg considers a primary culprit of HIV, Retrovir (AZT), ironically the first drug used to treat HIV (it actually isn’t ironic at all, when you learn the full history).



AZT looks an awful lot like thymidine, doesn’t it? That’s what it hopes your dumb ol’ cells think too when they take it on up. The idea is that the Azido group makes the sucker more lipophilic so it enters into the various membranes. Once it gets incorporated into the reverse transcriptase machinery the loss of the hydroxyl means no more chain elongation and thus it terminates the growing chain. (As you know, the chain growth is a result of forming a new Phosphodiester bond across those alcohols in thymidine.) This would ideally stop cell proliferation in cancer cells, but it didn’t… so it was shelved after being discovered in the 60’s. The original Big Evil Pharma, Glaxo Wellcome, stumbled upon the drug in the 1980’s. Since then it has been maliciously saving lives. [ This, more than anything, gave the drug industry a black eye. It is generally looked down upon when you refuse to sell a life saving medication to a country because they can’t afford it, - especially when it was discovered using federal grant money. HUGE PR nightmare.] Anyway, HIV is an RNA virus so it must first convert the RNA to DNA and it does so using its own brand of reverse transcriptase, which is carries along in its capsid. There you have it, an awesome antiviral. It totally screws up the viral reverse transcriptase by clogging it up with what the poor little guy thought was a thymidine. It does, however, fuck you up a little in the process.



In 2004 AZT raked in 1.8 billion dollars and is enjoyed in every corner of the world. It is now available as a generic. You can make your own, actually. It’s pretty easy to make, if you have some D-Mannitol handy.

0 comments: