In order to fight cancer, you must know as much as you can about the molecular workings of cancer growth. Scientists from the Florida campus of The Scripps Research Institute (TSRI) have shown how small, radically imperceptible structural changes in a key breast cancer receptor are directly linked to regulating molecules and can produce predictable effects in curbing or accelerating cancer growth. Published recently in the journal Molecular Systems Biology, this predictive statistical approach moves science one step closer to the development of more effective structure-based drug design to treat this disease. One of their long-term goals is to be able to predict proliferative or anti-proliferative activity of receptor molecule complexes by identifying structural changes that lead to specific outcomes.
Nettles and his colleagues synthesized more than 240 estrogen receptor binding molecules that led the cancer to proliferate, using structural analysis to determine the basis for receptor activity in identifying the root of estrogen reception (ERa) cells.
Research Proves Tamoxifen Can Cause Cancer
Many drug target-signaling proteins like the estrogen receptor tamoxifen (Nolvadex, AstrZeneca) that blocks the estrogen receptor’s proliferative effects of naturally occurring estrogen in breast cancer cells, can increase the risk of uterine cancer. Co-first author, Sathish Srinivasan, of the study with Research Associate Jerome Nwachukwu, pointed out the research suggests that certain structural changes might be made to the binding pocket to eliminate this negative side effect. Tamoxifen can have different effects in different tissues because of structural changes often not discernable using traditional methods. The team solved the atomic structure of some 76 different estrogen receptor-ligand complexes to better understand these responses.
Some of these effects can be predicted by measuring the distance between two specific carbon atoms of the estrogen receptor.
In conclusion they believe this is the first time they have been able to use these atomic structures to identify how very small changes from the ligands give different outcomes, leading us towards the goal of predicting which ligands are going to make the most effective treatments for breast cancer.
Wouldn’t it be great to make this leap forward in predicting cell changes that might affect breast cancer growth? Opening up more doors to effective therapies is another step towards defeating, or at least, trying to control the growth of this horrible cancer that plagues so many women (and men).