REVIEW PAC-1 (first procaspase activating compound) is a synthesized chemical compound that selectively induces apoptosis, or cell suicide, in cancerous cells. It is a small molecule compound that directly activates procaspase-3 to caspase-3 in vitro and induces apoptosis in cancerous cells isolated from primary colon tumors in a manner directly proportional to the concentration of procaspase-3 inside these cells. PAC-1 retarded the growth of tumors in three different mouse models of cancer, including two models in which PAC-1 was administered orally. PAC-1 is the first small molecule known to directly activate procaspase-3 to caspase-3, a transformation that allows induction of apoptosis even in cells that have defective apoptotic machinery. The direct activation of executioner caspases is an anticancer strategy that may prove beneficial in treating the many cancers in which procaspase-3 concentrations are elevated. PAC-1 restore procaspase-3 activity through the chelation of inhibitory zinc ions in vitro, induce apoptotic death of cancer cells in culture, and reduce tumor burden in vivo.
REFERENCES
[1]
Karson S Putt, Grace W Chen, Jennifer M Pearson, Joseph S Sandhorst, Martin S Hoagland, Jung-Taek Kwon, Soon-Kyung Hwang, Hua Jin, Mona I Churchwell, Myung-Haing Cho, Daniel R Doerge, William G Helferich & Paul J Hergenrother, Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy Nature Chemical Biology 2, 543 - 550 (2006).
[2]
Kovacic, Peter Does Structural Commonality of Metal Complex Formation by PAC-1 (anticancer), DHBNH (anti-HIV), AHL (autoinducer), and UCS1025A (anticancer) Denote Mechanistic Similarity? Signal Transduction and Medical Aspects, Journal of Receptors and Signal Transduction (2008), 28(3), 141-152.
[3]
Peterson, Quinn P.; Goode, David R.; West, Diana C.; Ramsey, Kara N.; Lee, Joy J. Y.; Hergenrother, Paul J. PAC-1 Activates Procaspase-3 in Vitro through Relief of Zinc-Mediated Inhibition Journal of Molecular Biology (2009), 388(1), 144-158.
[4]
West, Diana C.; Qin, Yan; Peterson, Quinn P.; Thomas, Diana L.; Palchaudhuri, Rahul; Morrison, Karen C.; Lucas, Pamela W.; Palmer, Amy E.; Fan, Timothy M.; Hergenrother, Paul J. Differential Effects of Procaspase-3 Activating Compounds in the Induction of Cancer Cell Death, Molecular Pharmaceutics (2012), 9(5), 1425-1434.
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