Unlocking the Secrets of Anti-Aging and Anti-Cancer Therapeutics

Published on December 7, 2022

Imagine you’re a treasure hunter on a quest for the ultimate fountain of youth and the ultimate weapon against cancer. Well, scientists have discovered some promising leads in their search for anti-aging and anti-cancer therapeutics. The most famous candidate in this search is a drug called rapamycin. It has shown great potential in slowing down the aging process, but it has one flaw – its physical properties make it less effective. So, researchers set out on a virtual journey to find new compounds that can inhibit a protein called mTOR, which is crucial for aging and cancer. They used advanced screening techniques and found seven lead compounds. After extensive testing, one compound called 3 showed remarkable abilities to kill cancer cells, rejuvenate normal cells, and inhibit mTOR directly. This compound even showed promise of reducing age-related cell damage. It’s like finding a golden key that unlocks the secrets of both fighting cancer and slowing down aging. Now, scientists are excited to further investigate compound 3 and see if it can truly become a powerful weapon against these two formidable foes! To learn more about this incredible research, check out the full article.

To date, the most studied drug in anti-aging research is the mTOR inhibitor – rapamycin. Despite its almost perfect anti-aging profile, rapamycin exerts one significant limitation – inappropriate physicochemical properties. Therefore, we have decided to utilize virtual high-throughput screening and fragment-based design in search of novel mTOR inhibiting scaffolds with suitable physicochemical parameters. Seven lead compounds were selected from the list of obtained hits that were commercially available (4, 5, and 7) or their synthesis was feasible (1, 2, 3, and 6) and evaluated in vitro and subsequently in vivo. Of all these substances, only compound 3 demonstrated a significant cytotoxic, senolytic, and senomorphic effect on normal and cancerous cells. Further, it has been confirmed that compound 3 is a direct mTORC1 inhibitor. Last but not least, compound 3 was found to exhibit anti-SASP activity concurrently being relatively safe within the test of in vivo tolerability. All these outstanding results highlight compound 3 as a scaffold worthy of further investigation.

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