Promising method new drugs are looking into
 

Any comments on this "new" way that drugs would work?

"Cell Surfaces

Drugs work by interacting with protein molecules that sit on the surfaces of cells. Binding, or receptor, sites have a specific structure and chemicals have to fit precisely onto these spots in order to bind to a protein and turn it on or off and have an effect. Mutel and his colleagues tried to find medicines that would attach to a G-protein coupled receptor -- a type of protein active in almost every organ system in the body -- for glutamate.

The team discovered a compound that fit to the receptor's so-called allosteric site, rather than the point that most modern drugs target. This allowed the chemical to modulate the glutamate receptor's activity rather than just switching it on.

``One of the biggest difficulties in drug development is that if you completely block or activate the body's own chemical systems, it can lead to side effects,'' Mutel, 50, said in an interview. ``What we're doing is not to turn the body's own systems on or off like a normal light switch, as most drugs do, but to control the amount of light in the room like a dimmer.''

`Lab Curiosity'

The drug also kicked into action only when the body's own messengers signaled a need, more closely mirroring the peaks and troughs of the body's own systems. The receptor's allosteric site was unusual in structure, making the medicine that fit it less likely to bind to and affect other proteins.

``With a typical drug on the market, if you want to target a particular site on a protein in the brain, the drug will also target the same site on a related protein in the heart,'' Christopoulos said. ``It's like turning on all the lights in the house when you just want to turn on the light in the kitchen.''

Except for the work on Amgen's Sensipar, modulating the receptors in this way had been considered a ``lab curiosity,'' Mutel said. The discoveries at Roche and crosstown rival Novartis in 2001 ``completely changed the whole perception of the field,'' he said.

Such development now focuses mostly on diseases of the brain and central nervous system. Addex has two drugs in human studies, the most advanced of which is in the second of three stages of testing generally needed for approval...."

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