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Tuesday, September 24, 2019 11:51:30 AM
Will Anavex own this process?
Well, could there be other, yet undiscovered molecules that could fit into the sigma-1 receptor protein and provide competing, favorable therapeutic outcomes? Not very likely.
First, the useful fit of the Anavex molecules into the sigma-1 receptor protein is essentially a lock-and-key arrangement. There must be a perfect fit. Unless a molecule has a perfect configuration, both physical and chemical (parallel binding sites), the molecule simply bounces off, fails to bind and can have no downstream effects.
The Anavex biochemists parsing the molecular configurations of their sigma-1 receptor agonists, starting with Anavex 2-73, continuing to Anavex 3-71 and all of the others, revealed or yet only on computer graphics, know full well which molecules can both bind to and be usefully effective on sigma-1 receptor proteins. I’m certain that if there were any other molecules that could effectively bind to the proteins, Anavex would have patented them.
Sure, other molecules will be able to bind to the involved active sites. No big deal. Many or most poisons bind effectively and preferentially to the active sites of essential enzyme proteins. But instead of facilitating the normal, useful chemical activity of the enzymes, they are poisoned; disabled. Being able to bind to a molecule does not necessarily make it work better. Quite the opposite. It disables the molecule, making it reactively inert, unable to control or affect downstream reactions.
So, yes, there are certainly other molecules that could bind to sigma-1 receptor proteins. But unlike the Anavex molecules, they would merely poison things; not make things better.
And just important is the ability of a drug molecule to get itself inside a cell to function there. Cells, especially neurons, expend great amounts of energy and have complex chemical systems the prevent entrance or energetically expel foreign, alien molecules. Wonderfully, the Anavex molecules are regarded by cells as natural; are not significantly excluded or expelled. Other molecules that might work are likely to be expelled or excluded.
For me, that was a remarkable finding of the recently released Rett clinical trial. The young women with Rett syndrome experienced strong therapeutic results regarding two factors: a) results appeared very quickly, in a few days or weeks, and b) they were treated with only 5mg of Anavex 2-73. That means that virtually all of the ingested drug (per oral, by mouth) got diffused into neurons. No rejection, either in the gastrointestinal organs, or in neurons themselves. Nothing better in drug administration.
I have no concern that some biochemist at some other pharmacological is going to come up with an Anavex competitor. Anavex, indeed, owns the technology.
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