A team at the National Health Research Institutes (NHRI) has discovered a novel orally available small molecule, DBPR728, that can cut off the nutrient supply for cancer cell growth, which can serve as a new targeted therapy drug.
The research team consists of scientists from the NHRI’s Institute of Biotechnology and Pharmaceutical Research, including Chi Ya-hui (紀雅惠), Yeh Teng-kuang (葉燈光), Chen Chiung-tong (陳炯東) and Chang Chun-ping (張竣評).
Chi told a news conference at the Ministry of Health and Welfare in Taipei yesterday that the occurrence of cancer is often caused by genetic aberrations that lead to uncontrolled cell proliferation.
Photo: Chen Yi-kuan, Taipei Times
An “oncogene” is a gene that has the potential to transform normal cells into cancerous ones through genetic aberrations — including mutation, fusion and amplification, she said.
Genetic amplification refers to an increase in the number of copies of the same gene, and studies have suggested that approximately 28 percent of cancers exhibit Myelocytomatosis (MYC) oncogene amplification, Chi said, adding that they include lung cancer, breast cancer, liver cancer and prostate cancer, as well as several other types.
For cancer cells to grow, the MYC oncoprotein functions as a transcription factor, facilitating the production of enzymes required for glycolysis (the process of breaking down glucose to produce energy), she said.
Therefore, MYC overexpression (too many copies of the MYC oncoprotein) allows cancer cells to metabolize energy in low-oxygen conditions, leading to uncontrolled cell growth and high post-operative recurrence rates, ultimately reducing overall patient survival rates, she said.
However, while there are many therapies that target specific genetic mutations in cancer cells, there are still challenges in developing drugs that target several oncogenes and their cancer-driving proteins, such as the MYC oncogene, due to the intrinsic properties of its proteins, Chi said.
In an effort to suppress MYC overexpression, Chi said the team tried to exploit its “good friend,” the enzyme Aurora kinase A, which stabilizes the MYC protein, by designing small molecules that disrupt the interaction between the two proteins, leading to MYC protein degradation.
They used the molecule DBPR728 to create an inactive oral drug that is stable in the gastrointestinal tract and can be bioconverted to become active when it reaches tumor cells, she said.
Chi said administering the oral drug to mice which have tumor cells with MYC genetic amplification and overexpression showed that the drug to can efficiently induce MYC reduction and cell apoptosis (the process of programmed cell death) in just 10 days.
The drug has obtained a patent in Taiwan and the team is applying for patents in other nations, and hopefully after it passes preclinical toxicity studies and clinical trials, it can be produced as a targeted drug for cancer treatment, she said.
The team’s findings were published in the June issue of Molecular Cancer Therapeutics, a leading journal published by the American Association for Cancer Research.
US President Donald Trump yesterday announced sweeping "reciprocal tariffs" on US trading partners, including a 32 percent tax on goods from Taiwan that is set to take effect on Wednesday. At a Rose Garden event, Trump declared a 10 percent baseline tax on imports from all countries, with the White House saying it would take effect on Saturday. Countries with larger trade surpluses with the US would face higher duties beginning on Wednesday, including Taiwan (32 percent), China (34 percent), Japan (24 percent), South Korea (25 percent), Vietnam (46 percent) and Thailand (36 percent). Canada and Mexico, the two largest US trading
AIR SUPPORT: The Ministry of National Defense thanked the US for the delivery, adding that it was an indicator of the White House’s commitment to the Taiwan Relations Act Deputy Minister of National Defense Po Horng-huei (柏鴻輝) and Representative to the US Alexander Yui on Friday attended a delivery ceremony for the first of Taiwan’s long-awaited 66 F-16C/D Block 70 jets at a Lockheed Martin Corp factory in Greenville, South Carolina. “We are so proud to be the global home of the F-16 and to support Taiwan’s air defense capabilities,” US Representative William Timmons wrote on X, alongside a photograph of Taiwanese and US officials at the event. The F-16C/D Block 70 jets Taiwan ordered have the same capabilities as aircraft that had been upgraded to F-16Vs. The batch of Lockheed Martin
GRIDLOCK: The National Fire Agency’s Special Search and Rescue team is on standby to travel to the countries to help out with the rescue effort A powerful earthquake rocked Myanmar and neighboring Thailand yesterday, killing at least three people in Bangkok and burying dozens when a high-rise building under construction collapsed. Footage shared on social media from Myanmar’s second-largest city showed widespread destruction, raising fears that many were trapped under the rubble or killed. The magnitude 7.7 earthquake, with an epicenter near Mandalay in Myanmar, struck at midday and was followed by a strong magnitude 6.4 aftershock. The extent of death, injury and destruction — especially in Myanmar, which is embroiled in a civil war and where information is tightly controlled at the best of times —
China's military today said it began joint army, navy and rocket force exercises around Taiwan to "serve as a stern warning and powerful deterrent against Taiwanese independence," calling President William Lai (賴清德) a "parasite." The exercises come after Lai called Beijing a "foreign hostile force" last month. More than 10 Chinese military ships approached close to Taiwan's 24 nautical mile (44.4km) contiguous zone this morning and Taiwan sent its own warships to respond, two senior Taiwanese officials said. Taiwan has not yet detected any live fire by the Chinese military so far, one of the officials said. The drills took place after US Secretary
RSS