PAC-1

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PAC-1

PAC-1 is a procaspase-activating compound that was first identified in 2006. It is a small molecule that can induce apoptosis in cancer cells by activating procaspase-3, leading to the production of the active caspase-3 enzyme. This enzyme plays a crucial role in the execution-phase of cell apoptosis, or programmed cell death.

History

The discovery of PAC-1 was first reported in 2006 by a team of researchers at the University of Illinois at Urbana-Champaign. The team was led by Paul J. Hergenrother, a professor of chemistry. The discovery was a significant breakthrough in the field of apoptosis research, as it provided a new approach to induce cell death in cancer cells.

Mechanism of Action

PAC-1 functions by chelating essential zinc ions from the procaspase-3 enzyme. This chelation process activates the enzyme, leading to the initiation of apoptosis. The ability of PAC-1 to directly activate procaspase-3 distinguishes it from other apoptosis-inducing agents, which typically function by disrupting the balance between pro- and anti-apoptotic signals within the cell.

Clinical Trials

As of 2021, PAC-1 has been evaluated in several clinical trials for its potential use in cancer treatment. These trials have primarily focused on the treatment of glioblastoma, a type of brain cancer, and lymphoma, a type of blood cancer. The results of these trials have shown that PAC-1 is well-tolerated and has potential anti-cancer activity.

Future Directions

Research is ongoing to further understand the potential applications of PAC-1 in cancer treatment. This includes studies to determine the optimal dosing and administration methods, as well as investigations into potential combination therapies with other anti-cancer agents.

See Also

• Apoptosis
• Caspase
• Clinical trial
• Glioblastoma
• Lymphoma
• Paul J. Hergenrother
• Zinc