Medicinal Chemist, Professor Patrick Gunning targets on his latest research to design a molecule that targets a cancer-promoting protein called STAT3. For the last three years from 2016, Gunning has developed a powerful family of molecules that disable the STAT3 protein and stops the spread of numerous cancers while leaving the healthy cells untouched. STAT3 is coined as a master regulator of the cancer cell. How does drugs works on our body. As organic chemist thinks that our body is made of connection.
Why does the cancer cell like to grow, expand and evade?
This is controlled by beautiful caskets of protein. Protein interactions that leads to genes being produced that tell the cell what to do. And in cancer these genes are telling it to survive and to grow. STAT3 expresses genes that leads to division, growth and preventing cell death.
How can we target STAT3 if it’s already performing a normal role?
For normal cells STAT3 is switched on for a very short period of time and quickly shut down. Cancer cells are permanently switched on. And because it’s permanently switched on you have this all expression genes that leads to the cancer cells. Medicinal chemistry targets STAT3. Medicinal chemistry perspective is the design and senses of small, typically organic molecules that binds to specific protein with the exquisite selectivity and potency. And the result of the interaction is the biological response and in cancer that has to be cell death. We won’t let the interaction lead to cell death. In STAT3 they found 3 main binding site, in an active side of protein. Professor Gunning wanted to make a molecule that could access all of those sites. They used computational modelling to identify molecules that could bind.
IC50 is the concentration of a drug required to kills 50% of cancer cells. They bind the molecule to the proteins to see if it’ll bind and next one they bind it with cancer cells. They treat the cancer cell with the molecule to see if the hypotheses is correct by targeting the protein the cell is done. They want to see a molecule that is good to normal cell and cancer cell.
BP1102 which is .8 micromolar is the starting point. It was found out that it didn’t kill those cell and found out on breast cancer cells that it dramatically affected the great number of cells kills them.