Jung-Mo Ahn, PhD, associate professor of chemistry at The University of Texas at Dallas, has designed and synthesized a novel small molecule that might become a large weapon in the fight against prostate cancer.
In a study published online in the journal Nature Communications, Ahn and his colleagues at UT Southwestern Medical Center, including senior study author Ganesh Raj, MD, PhD, describe the rational design of the molecule, as well as laboratory tests that show its effectiveness at blocking the cancer-promoting function of proteins called androgen receptors. Androgen receptors are found inside cells and have complex surfaces with multiple “docking points” where various proteins can bind to the receptor. Each docking point has a unique shape, so only a correctly shaped molecule will fit.
Looking for a new approach to battle prostate cancer, the researchers keyed in on blocking a critical docking point on the androgen receptor. Using computer-assisted molecular modeling, they designed a helix-mimicking small molecule that fits precisely into a pocket on the androgen receptor that is associated with prostate cancer. The researchers tested the compound in animal and isolated human tissue. Without exhibiting noticeable toxicity, the compound prevented the androgen receptor from recruiting its protein partners and it blocked the growth of prostate cancer cells. Read the study abstract.