Another major breakthrough in targeted therapy

Thread Content

As times have changed, humanity’s struggle against cancer has moved from the ineffective approaches of the chemotherapy era to the era of precision targeted therapy. What is targeted therapy? As the name implies, it involves designing therapeutic drugs at the cellular and molecular level targeting the cancer-causing factors, thereby causing the tumor cells to die specifically, without affecting surrounding cells as chemotherapy does. Most of the targeted drugs available on the market or under investigation currently are kinase inhibitors; a small portion belong to another important class of targeted drugs: protein interaction inhibitors. Progress with these drugs has been slow, as the interaction surfaces of proteins are much larger than the range of action that small molecules can achieve, and there are few successful examples of such drugs to date. Not long ago, Professor Zhang Zhichao from Dalian University of Technology published a report on a dual-functional bcl-2-targeting anticancer lead drug developed by his team in the cover edition of a top international journal in the field of chemistry. This study reveals for the first time that a key protein in the Bcl-2 family protein complex possesses two functional conformations, an “on” state and an “off” state. It is also the first time that small molecules have been used to precisely drive this protein into its “off” conformation and lock it there, thereby regulating the signal transduction pathways in malignant tumors back to normal cellular levels. This approach enables the efficient and precise elimination of tumor cells, offering new targets and mechanisms for precision medicine in oncology. The above article is sourced from Molfind Web (www.molfind.cn)