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How the tilt of a cell-surface receptor prevents cancer
Date:1/31/2013

t its main function was as a marker for the point at which the receptor emerges from membrane into the cell's cytoplasm. "We think these tryptophans may be more than just border markers, that they may generally prevent the spontaneous activation of some receptors by impairing the close apposition of membrane coils," says Constantinescu. He and his colleagues have begun bioinformatics studies to test this hypothesisand determine if similar mutations on other single-pass receptors are also associated with cancer.

The current findings could have implications for cancer drug development as well. Constantinescu's lab has already established a partnership with a group at the Experimental Therapeutics Center in Singapore to develop experimental methods to rapidly evaluate the ability of small molecules to force membrane-embedded coils of mutated TpoR to return to their normal, tilted position. "Such molecules," says Constantinescu, "could have some potential as cancer therapeutics."


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Contact: Rachel Steinhardt
rsteinhardt@licr.org
212-450-1582
Ludwig Institute for Cancer Research
Source:Eurekalert

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