Word: receptor
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...turns out that COX-2 inhibitor drugs also have anticancer effects, reducing the number of precancerous polyps in patients with a hereditary form of colon cancer, perhaps through antiangiogenesis. Scientists are currently studying its effect on noninherited colon cancers. And because the receptor for COX-2 is overexpressed on a range of human cancer types, the hope is that COX-2 inhibitors may be useful in preventing a wider range of cancers, including head and neck, bladder, non-small cell lung and breast cancers...
...more modest expectations. Rituxan was the first, but just a year later, the same approach led to Herceptin, a drug that keeps growth factors from feeding certain kinds of breast-cancer cells. Such targeted treatments are effective only when the appropriate target exists. Herceptin, for example, latches onto a receptor known as HER2, which is abnormally abundant in only about 30% of breast-cancer tumors. A biopsy can tell doctors whether a patient is likely to respond to Herceptin, but they'd hoped to find a molecule that would plug into a growth-factor receptor more prevalent in cancer cells...
Sure enough, they found one. Dr. John Mendelsohn, then at the University of California, San Diego, and now president of the M.D. Anderson Cancer Center in Houston, had been focusing since 1981 on a receptor called EGFR, which is host to a protein called epidermal growth factor (EGF). It's a close cousin to HER2, and Mendelsohn and his team know that it is present in a huge variety of tumors; two-thirds of all cancer types, in fact, are blanketed with EGF receptors. In 1984 Mendelsohn and his team showed in mice that blocking the EGF receptor with...
Making a drug out of that decoy would prove tricky, since the receptor, like HER2, also shows up on noncancerous cells. Researchers are now learning, however, that normal cells are more adept than cancer cells at finding other growth factors on which to rely when EGFR is blocked. But when Mendelsohn applied for his first grant from the National Cancer Institute in 1983, he was rejected. "Nobody thought it would work," he says. The following year he turned to philanthropic sources for research dollars. Last year he wowed colleagues with a compound called IMC-C225, which proved effective in treating...
...turns out that COX-2 inhibitor drugs also have anticancer effects, reducing the number of precancerous polyps in patients with a hereditary form of colon cancer, perhaps through antiangiogenesis. Scientists are currently studying its effect on noninherited colon cancers. And because the receptor for COX-2 is overexpressed on a range of human cancer types, the hope is that COX-2 inhibitors may be useful in preventing a wider range of cancers, including head and neck, bladder, non-small cell lung and breast cancers...