Word: inhibitor
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...that inhibits ACE-2. Scientists combed through Millennium's library of 700 different classes of compounds for molecules whose chemistry made them candidates to clamp down on ACE-2 activity. Then, with the help of protein-modeling software (see Bioinformatics box), they manipulated the chemical structure of their new inhibitor to give it optimal binding affinity with the ACE-2 receptor. In about two years, Millennium had created a new blood-pressure-drug candidate that is now being tested in animals...
...last step for the ACE-2 inhibitor, as for any drug, is human clinical trials. Because the Food and Drug Administration requires such rigorous testing, this is by far the most expensive part of drug development. So for human trials in some cases, Millennium has formed partnerships with large pharmaceutical companies that have the necessary resources and will share in any eventual profits...
ALZHEIMER'S DISEASE Scientists began safety testing the first drug designed to tackle the root cause rather than the symptoms of this brain-addling disease. Patients in the early stages of Alzheimer's were given a gamma secretase inhibitor, a compound that blocks the formation of the sticky plaques that gum up the brain's neural connections. So far, the drug seems to have been well tolerated...
Trimeris' compound, called T-20, blocks the final structural contortion from taking place. For this reason it and a second candidate, T-1249, are known as fusion inhibitors. Progenics has been testing a different type of entry inhibitor, a molecular decoy for CD4 whose job is to find, bind and lure HIV away from the real CD4 cells...
Last year one of these highly refined derivatives became the first so-called secretase inhibitor to enter clinical trials with Alzheimer's patients, and others seem sure to follow. In fact, not just Bristol-Myers Squibb but also Amgen, Elan Pharmaceuticals, Eli Lilly, Merck and SmithKline Beecham are racing to develop similar compounds. The reason? Over the past five years, an explosion of insights into the genetics of Alzheimer's has bolstered confidence that gamma secretase and a related enzyme called beta secretase are not innocent bystanders but rather are intimately involved in the disease process...