cancer researcher UC Santa Cruz receives $ 350,000 to develop new drugs for breast cancer -
UC Santa Cruz researcher Seth Rubin cancer received a grant of $ 350,000 to fund its work towards the development of a new class of drugs for breast cancer treatment. The grant is a Cancer Research Award program in breakthrough medical research programs led by the Congress of the US Department of Defense.
Rubin, an associate professor of chemistry and biochemistry, will use the grant to build on recent discoveries regarding a key protein tumor suppressor that is inactivated in most breast cancer cells. The retinoblastoma tumor suppressor protein (Rb) helps regulate the cycle of cell growth and division, putting the brakes on cell proliferation when it is active. In normal cells, Rb coordinates cell growth signals, turn on and off to ensure that the cells divide at the right time. The genetic changes in cancer cells disrupt this regulation and allow cells to multiply out of control.
Rubin's research revealed important details of the molecular mechanisms involved in the Rb transformation on and off. These results suggest the possibility of a new class of therapeutic molecules that target the retinoblastoma protein directly. Most attempts to target the path of retinoblastoma with drugs have focused on blocking the action of other proteins which inactivate Rb.
"A common analogy is to think of cancer cells as being like a car with a stuck accelerator and broken brakes, so the cells can not stop the proliferation. Most drugs target the accelerator stuck and down proteins that are active too. We want to target the broken brakes and restore tumor suppressor activity, "said Rubin.
This new approach promises to have fewer side effects toxic and less susceptible to acquired drug resistance than other therapies. drug discovery efforts Traditional focus on finding molecules that block the activity of a target protein. Little attention has been given to help small molecules to activate a tumor suppressor directly. the search Rubin could open a new class of targets for drug discovery efforts.
Rubin laboratory has developed a test Rb activity to use in large-scale testing procedures to identify small molecules that can stabilize the activated form of Rb. Identify molecules with the desired activity is the first step in the drug development process and requires very large number of screening compounds.
Rubin used a small grant from the Group Santa Cruz Cancer Benefit (SCCBG), a charitable cancer supporting local research and patient care, to test the Rb dosage of his group in a pilot study in UCSC chemical screening center. Their driver screen about 20,000 compounds showed that the test works well in a high throughput screening procedure.
The new grant will fund a collaboration with the Centre Conrad Prebys Chemical Genomics at Sanford-Burnham Medical Research Institute in La Jolla. The center will use the Rubin test to screen a library of approximately 320,000 compounds. Tracking studies to further evaluate compounds identified in large-scale screening tests will be carried out by the laboratory in collaboration with Rubin Julien Sage, a cancer biologist at the Stanford School of Medicine.
Rubin's lab also will investigate the molecular details of how lead compounds interact with the retinoblastoma protein. These studies provide a basis for future work needed to develop promising compounds in medically useful drugs for breast cancer treatment.
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