SLAC X-rays help discover new drug against melanoma

SLAC X-rays help discover new drug against melanoma

4:56 PM, 22nd July 2011
SLAC X-rays help discover new drug against melanoma
While malignant melanoma accounts for less than 5 percent of all skin cancers, it is the most aggressive and deadly, killing nearly 9,000 Americans this year, according to the American Cancer Society, © Plexxikon Inc.

MENLO PARK, US: 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.

Plexxikon’s success, reported last month, is an impressive victory for an emerging approach to combating illness: creating drugs custom-designed to throw molecular monkey wrenches into the disease process.

First researchers identify a target protein that plays a key role in the disease. In this case, it was an enzyme involved in cell growth that sometimes mutates and makes cells multiply out of control, the hallmark of cancer. If the scientists could find a small molecule that fits perfectly into a specific place in the mutated enzyme, they could block the enzyme’s action and slow or stop the cancer.

The researchers screen hundreds of small molecules - potential drugs - and identify the most promising ones. The technique, known as macromolecular X-ray crystallography, has become an important tool for probing large, complex biological molecules and discovering new drugs.

Plexxikon also used the X-ray crystallography facilities at SLAC’s Stanford Synchrotron Radiation Lightsource (SSRL), to design two other drugs that are now being tested in humans. “Structures produced by X-ray crystallography provide precise information on how a drug interacts with its protein target. This information enables a small chemistry team to generate new drug candidates quickly,” said Chao Zhang, Head of Structural Chemistry, Plexxikon. Also, Macromolecular crystallography is a rapidly growing activity.

“Ten years ago we could typically examine only 20 crystals per 8-hour shift on a beamline and collect data from one or two of them,” said Ana Gonzalez, Senior Staff Scientist, SSRL. Now, she said, users can manipulate their samples and measure the data remotely, over the Internet, “And during a single shift we can look at some 100 crystals and also collect datasets from 20 to 30 of them.”

The future offers potentially transformative new technologies thanks to SLAC’s Linac Coherent Light Source or LCLS. By enabling scientists to determine the structures of many proteins that don’t fully crystallize, “The ultrafast LCLS X-ray beam has the potential to guide the design of next-generation drugs,” said Plexxikon’s Zhang.

(C) SLAC National Accelerator Laboratory News

 

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