Oxford University Researchers See Promise In Elegant, Novel Ebola Knock-Out Approach

First — the scientific caveats: there is no evidence yet that this effect will persist in other mammals, or in fact, in a human model. So, these are clearly the quite early days. But they are encouraging ones, just the same.

It seems a near certainty that future research, and researchers, will find small-molecule compounds that bind more elegantly to this pocket, than ibuprofen does. Even so, it is exciting that at least one small molecule — one well-understood, and well-tolerated by humans — binds to this pocket (and is a well vetted, common pain-reliever). [Regular readers here know that Merck’s vaccine is highly effective, but reliable treatments for acute cases don’t yet exist.]

Indeed, I’d say it’s worth a read of the whole article in Nature, via this summary at Chemical and Engineering News — and here’s a bit of it:

. . . .Researchers led by Oxford University’s David Stuart solved the structure of the virus glycoprotein to a resolution of 2.2 Å in complex with two different molecules that scientists have shown can reduce infection in rodents: ibuprofen and the chemotherapy drug toremifene. . . .

When the Ebola virus infects a host cell, the first thing it does is attach itself to the cell using a glycoprotein. A newly obtained structure of that glycoprotein — the highest resolution one to date — now reveals a vulnerability in the virus’s infection machinery. Given the lack of approved therapies to combat the virus, this work gives medicinal chemists a weak point to target as they try to design molecules that stop Ebola’s deadly spread. . . .

Stuart’s team found that both chemicals bind in a buried pocket of the virus glycoprotein. The binding of these chemicals likely pushes the glycoprotein prematurely into a state where it can’t infect host cells, Stuart says. . . .

It is often the simplest answers that are the most elegant. We will hope to be back much later on the Fourth, with updated news from Jupiterif all the Universe’s forces align on this coming 2016 Independence Day evening. Smile. . . .


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