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Scientists Discover New Strategy to Fight Cancer Drug Resistance

by Kathy Jones on June 21, 2010 at 9:44 PM
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 Scientists Discover New Strategy to Fight Cancer Drug Resistance

A way to immobilize a common protein that often opposes chemotherapy treatment of various forms of cancer has been discovered by scientists.

The researchers have discovered that that they could exploit a small portion of the protein, called MCL-1, to make a molecular tool that hindered MCL-1's "pro-survival" action.

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Prototype drug blocks MCL-1 protein that helps tumours survive treatment

"We think this is a very important step toward developing an inhibitor of MCL-1, which is emerging as a critical survival factor in a broad range of human cancers, including leukemia, lymphoma, multiple myeloma, melanoma, and poor-prognosis breast cancer to name just a few," Nature quoted Dr. Loren Walensky, a paediatric oncologist and chemical biologist at Dana-Farber and Children's Hospital Boston.
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Walensky said that molecular mimics of these domains are showing great promise in early clinical trials, yet most of these drugs block three or more BCL-2 family proteins, rather than homing in on one specific cancer-causing target.

"An ideal pharmacologic toolbox would contain agents that target individual BCL-2 family proteins, subsets, and all members," explained Walensky, who is also an assistant professor of paediatrics at Harvard Medical School.

The Dana-Farber researchers were also able to analyse the three-dimensional structure of the key parts of the MCL-1 docking mechanism and discover why it binds so specifically to its target.

"Our data provide a blueprint for the development of novel therapeutics to reactive apoptosis in diseases driven by pathologic MCL-1-mediated cell survival and chemoresistance," they wrote.

The findings of the study were published on the Nature Chemical Biology website.

Source: ANI
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