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Biotech / Medical : Geron Corp.

GERN 1.370

-2.1%

Dec 26 9:30 AM EST

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To: seminole who wrote (523)	8/25/1997 4:01:00 PM
From: Rob-Chemist	of 3576

If possible, companies generally like to start by screening compounds against a pure enzyme simply because it is cheaper. To screen cells for a specific "anti-telomerase" effect would be rather expensive since you would have to assess the telomere length in each assay. These whole cell assays would be advantageous, however, since you might discover compounds that inhibit telomere synthesis by mechanisms other than telomerase inhibition. Once a company gets a compound that inhibits the purified telomerase protein, then they can consider its effects in whole cells. If needed, the compound can often be synthesized as a prodrug that more easily passes through the cell membrane, or if needed, is more water soluble. The prodrug will often be activiated once in the cell. A classic example of this approach is dideoxyinosine (DDI) used for treating HIV infection. The DDI must first be converted to the adenosine analog and then phosphorylated to the triphosphate for activity. At a conference on nucleosides a couple years ago, I had heard a rumor that some company had a good telomerase inhibitor. However, I have heard nothing more about the compound so I suspect the rumor was false and/or premature.

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