Cells continue to use molecular switches (phosphate molecules) to turn protein expression on and off, and as such, this molecular switch has become a common drug target. In a new study, the researchers found that direct activation of a tumor suppressor protein with a new small molecule prevented lung cancer from growing in mice. The relevant research results were published in the Journal of Clinical Investigation on May 15, 2017, and the title of the paper is "Activation of tumor suppressor protein PP2A inhibits KRAS-driven tumor growth". Dr. Goutham Narla of Case Western Reserve University in the United States said, "All of the drugs we currently have to treat our cancer patients are targeted kinases, enzymes that attach phosphate molecules to proteins. But, just as important, There is an enzyme that removes the phosphate molecule (ie, phosphatase)." A phosphatase called PP2A is able to shut down their expression by removing phosphate molecules attached to tumor proteins. However, according to Dr. Narla, "The expression of this tumor suppressor protein is turned off in almost every major cancer. Its inactivation is essential for normal cells to become cancer cells." Narla and his team decided to adopt an unconventional approach to cancer drug development: look for molecules that directly target PP2A in order to reactivate its tumor suppressive properties. A total of 54 researchers screened whether a series of drug-like molecules could reactivate PP2A in lung cancer cells and prevent lung cancer tumor growth in mice. The researchers found that a specific prototype drug can attach to a subunit of the PP2A protein, effectively activating the enzyme. As Dr. Narla explained, this study is the first to use a small molecule to directly activate an enzyme that removes phosphate molecules. In laboratory models, including preclinical lung cancer cell models and mouse models, this prototype drug also prevents lung cancer cell proliferation. Mice receiving this prototype drug injection have fewer lung cancer tumors and do not experience weight loss or behavioral abnormalities associated with other cancer drugs. In a mouse model, the efficacy of this prototype drug is comparable to the current combination of drugs used to delay lung cancer progression. To confirm where this prototype drug binds to PP2A, these researchers also developed lung cancer cells with specific mutations at putative drug binding sites. Mice suffering from tumors produced by these mutant lung cancer cells did not benefit from this prototype drug because the prototype drug was unable to bind and reactivate PP2A. Narla notes, “About more than 2,000 papers explore the role of PP2A in cancer. In breast cancer, prostate cancer, lung cancer, brain cancer, childhood cancer, ovarian cancer, and endometrial cancer, every major cancer Involving the inactivation of this protein. It allows us to activate the molecules it expresses and has the potential to play a role in a range of cancer patients." Narla added, “We are testing our prototype drugs in a series of animal models. If things continue to progress well, then we hope to use this prototype drug for clinical trials next year. Our initial clinical trials will be more extensive. Will cover many different types of cancer patients, including lung cancer patients." The study was conducted in preclinical lung cancer cell models and mouse models, and the results obtained may not be applicable to human lung cancer. Furthermore, mice received lung cancer tumor transplants instead of producing the tumor themselves, and they received this prototype drug treatment for only four weeks. The long-term therapeutic effect of this prototype drug is still unknown. Shanghai Chuangsai Technology has excellent performance, interleukin cytokines, fetal bovine serum, electrophoresis equipment scientific instruments, raw material drug standards, chemical reagents, cell culture consumables, Shanghai Chuangsai, mass products special promotions, welcome to inquire!
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JCI: A prototype drug uses a new mechanism to treat lung cancer