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DOE Pulse
  • Number 342  |
  • July 25, 2011

SLAC X-rays help discover new drug against melanoma

Representation of a drug developed in part at SLAC at work against melanoma. (Image courtesy of Plexxikon Inc.)

Representation of a drug
developed in part at SLAC at
work against melanoma. 
(Image courtesy of
Plexxikon Inc.).

It was front page news around the world: a drug designed to disrupt malignant melanoma, the deadliest form of skin cancer, was so successful in its latest round of testing in humans that the tests were halted—like an early-round knockout in boxing—so patients in the trial who were receiving other treatments could be moved to the new medicine.

A crucial part of the research for developing this new drug, called vemurafenib, took place at three DOE national laboratories: SLAC National Accelerator Laboratory, Argonne National Laboratory and Lawrence Berkeley National Laboratory. A Berkeley-based drug-discovery company, Plexxikon, used the labs’ powerful X-ray facilities to determine the precise structure of a mutated protein involved in this cancer—and potential drug candidates that could stop its spread.

Researchers employed a technique known as macromolecular X-ray crystallography at SLAC’s Stanford Synchrotron Radiation Lightsource, using intense X-rays to probe large, complex biological molecules in the drug discovery process.  A rapidly growing activity at SLAC, six of SSRL’s 30 beamlines host a large number of such projects each year; the specialized beam lines are funded primarily by the Department of Energy’s Office of Biological and Environmental Research and the National Institutes of Health.

Plexxikon also used SLAC’s X-ray crystallography facilities at SSRL to design two other drugs that are now being tested in humans. One is aimed at type II diabetes and other metabolic disorders. The other attacks cells found in many metastatic breast, colorectal, lung, and prostate cancers, and may also be effective against autoimmune diseases such as rheumatoid arthritis, multiple sclerosis and lupus.

Plexxikon’s recent success in disrupting melanoma is an impressive victory for an emerging approach to combating illness: creating drugs custom-designed to throw molecular monkey wrenches into the disease process.

Submitted by DOE's SLAC National Accelerator Laboratory