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.
AdvertisementPrototype 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.
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.
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