For decades, scientists around the world have struggled to target MYC, a key protein notorious for driving some of the most aggressive and deadly forms of cancer. In a groundbreaking advance that could redefine cancer therapy, Oluwatosin Obisesan, a Nigerian-born scientist, has co-developed a novel compound, MY05, designed to disarm the MYC oncoprotein. This discovery marks a major step forward in the decades-long battle against tumors fueled by MYC.
In the peer-reviewed article titled “Discovery of a Pyrazolopyridinone-Based MYC Inhibitor that Selectively Engages Intracellular c-MYC and Disrupts MYC–MAX Heterodimerization”, published in the Journal of Medicinal Chemistry, Obisesan and her team introduce MY05, a small-molecule drug that engages MYC inside cells. The compound prevents MYC from binding to the MAX protein, halting a crucial partnership that promotes the expression of genes involved in cell proliferation and tumor growth.
Inside every cell in the human body, myriads of proteins help regulate how cells grow, divide, and function. Among these are MYC and MAX, which work together, acting as a master switch to turn on genes that encourage cells to multiply. When functioning normally, this system is tightly controlled, ensuring cells multiply only as needed. In many cancers however, MYC becomes overproduced and overactive, continuously instructing cells to divide even when they should not. This unregulated growth leads to tumor formation and rapid cancer progression.
For MYC to drive cell proliferation, it must form a complex with MAX, known as MYC–MAX dimerization. Because this interaction is essential for MYC’s cancer-causing activity, scientists have long sought ways to disrupt it. However, MYC is a notoriously tricky target for drug development due to its disordered shape, which makes it hard for drugs to bind. Hence the need for novel drugs and strategies to disrupt MYC-MAX heterodimerization.
The discovery of MY05 is an exciting development in the fight against cancer. The compound directly interferes with the MYC–MAX interaction, offering a promising way to shut down this major engine of cancer growth. What makes MY05 particularly promising is that it selectively targets MYC in cancer cells, sparing normal cells that are not heavily dependent on MYC.
“MYC protein has long been considered ‘undruggable’ due to its intrinsically disordered structure, posing a formidable challenge in cancer therapeutics,” says Obisesan. Her research shows that MY05 binds to MYC and prevents the formation of the MYC-MAX complex. This not only disrupts MYC’s function but also destabilizes the protein, reducing its levels inside the cell. As a result, the compound effectively halts cancer cell proliferation and tumor growth in preclinical models.
Although breast cancer cells were used primarily in the study, Obisesan notes that MY05 could potentially be effective in treating other cancers driven by MYC.
Beyond this groundbreaking work, Oluwatosin Obisesan has made significant contributions in her field through her drug discovery and development efforts. She has co-authored multiple studies focused on creating novel compounds for cancer therapy, demonstrating a strong commitment to scientific innovation and translational impact. Her work has earned her growing recognition in the field, including being named a Rising Star by the Sanford Burnham Prebys Cancer Center and awarded the Advancing Science Conference Grant from the National Organization for the Professional Advancement of Black Chemists and Chemical Engineers (NOBCChE).
Obisesan has also been celebrated for her efforts to advance health equity through research. In 2022, she was selected for a competitive two-year fellowship in the United in True Equity Research Priority Area (UNITE RPA) Predoctoral Research Enhancement Program at the University of Kentucky. This program supports innovative research dedicated to addressing health disparities, highlighting her exceptional research potential and commitment to scientific excellence.
Her work not only opens new avenues for cancer treatment but also exemplifies the power of inclusive, equity-driven scientific leadership.
The discovery of MY05, led by Obisesan, represents a major leap forward in the fight against cancer and brings renewed optimism to efforts targeting hard-to-treat tumors. By successfully inhibiting the elusive MYC protein, the research lays the foundation for a new generation of precision drugs that could benefit millions of patients worldwide. MY05 opens the door to treatments that were once considered impossible.
This success also underscores the importance of investing in bold, innovative science, and the vital role diverse scientific talents play in advancing global health. Obisesan’s work does not only mark a scientific milestone but also exemplifies the growing global impact of African-born researchers, offering inspiration to the next generation of trailblazing scientists
