Using the structure of the epidermal growth factor receptor to fight cancer

September 13, 2010
The fly EGFR as a 'two-stage switch'. Its structure is shown in three stages, left to right. At left, no growth factors are bound (off). However, as one (middle) and two (right) growth factors bind (shown in magenta) it sends two different signals

(PhysOrg.com) -- The protein EGFR, which is the target of several cancer drugs, has a split personality at the cell surface, with two different classes (high-affinity and low-affinity), whose origins have been a mystery since the 1970s. Now, a new paper by Penn researchers published in Cell explains the difference between these two classes.

This video is not supported by your browser at this time.

Many types of tumors grow because of over-expression or a mutation of a protein called the (EGFR), normally regulated by a hormone-like peptide called the epidermal growth factor (EGF). Several , including , Erbitux, Iressa and Tarceva fight tumors by blocking EGFR and related receptors, notes Mark A. Lemmon, PhD, Professor and Chair of Biochemistry and Biophysics at the University of Pennsylvania School of Medicine.

EGFR has a split personality at the , with two different classes (high-affinity and low-affinity), whose origins have been a mystery since the 1970s. Now, a new paper from the Lemmon lab published recently in Cell explains the difference between these two classes by examining the structure of EGFR and its interactions with EGF.

The researchers took advantage of unique properties of the fruit fly equivalent of human EGFR as a window into the molecules' structures. They found that the EGF receptor acts like a two-stage switch.

“Two growth factors can bind to the receptor that signals across the membrane,” explains Lemmon. “With no receptors bound, the receptor is fully off. But, it looks as if there is a different type of signal if just one of the sites is filled as compared to when EGF is bound to both.” Interestingly, the insulin receptor is known to have similar properties.

Explore further: Study reveals how some molecules inhibit growth of lung cancer cells

Related Stories

Protein inhibits cancer cell growth

December 21, 2009

(PhysOrg.com) -- Researchers at the University of Toronto and Goethe University in Germany have discovered a protein that can inhibit the growth of cancer cells, providing crucial clues for the future development of new drugs ...

Scientists show how brain tumors outsmart drugs

January 19, 2010

Researchers at the Ludwig Institute for Cancer Research (LICR) at the University of California, San Diego School of Medicine and Moores UCSD Cancer Center have shown one way in which gliomas, a deadly type of brain tumor, ...

Recommended for you

How the finch changes its tune

August 3, 2015

Like top musicians, songbirds train from a young age to weed out errors and trim variability from their songs, ultimately becoming consistent and reliable performers. But as with human musicians, even the best are not machines. ...

Machine Translates Thoughts into Speech in Real Time

December 21, 2009

(PhysOrg.com) -- By implanting an electrode into the brain of a person with locked-in syndrome, scientists have demonstrated how to wirelessly transmit neural signals to a speech synthesizer. The "thought-to-speech" process ...

0 comments

Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.