Cancer Cell: Scientists have discovered enzyme inhibitors that inhibit multiple tumors
March 29, 2016 Source: Bio Valley
Window._bd_share_config={ "common":{ "bdSnsKey":{ },"bdText":"","bdMini":"2","bdMiniList":false,"bdPic":"","bdStyle":" 0","bdSize":"16"},"share":{ }};with(document)0[(getElementsByTagName('head')[0]||body).appendChild(createElement('script')) .src='http://bdimg.share.baidu.com/static/api/js/share.js?v=89860593.js?cdnversion='+~(-new Date()/36e5)];Their research focus is on c-Myc tumor protein, which is expressed in nearly half of human tumors, and SIRT2-- an enzyme that plays a key role in the viability of many cancer cells. Using a compound called TM, the researchers can inhibit SIRT2 activity, reduce c-Myc protein levels, and inhibit tumor growth in a mouse model of breast cancer.
This research has taken us a step further on the road to healing the disease that kills 8 million people every year. Their work was published in the Cancel Cell magazine.
"This research starts with basic science and is the basic research that takes us on this path. It looks promising. We hope to develop effective anticancer drugs in the next few years," said Hening Lin, one of the authors of the study.
Previous studies of deacetylase inhibitors, including inhibitors of SIRT2, were limited by differences in availability and selectivity. Through research and developmentTM and three other analogs, Lin and colleagues found that TM has the best activity and selectivity for inhibiting SIRT2 protein. The team sent the TM to the National Cancer Institute to screen about 60 cancer cell lines. The results show that 10 uM TM can inhibit 36 ​​of 56 tumor cells by more than 50%, including all leukemia cell lines and most rectal cancer cell lines.
Lin said: "This discovery is actually a bit surprising. We were originally targeting the SIRT6 protein when we made TM compounds." SIRT6 is another enzyme in the deacetylase family.
Based on two previous studies, SIRT2 was thought to be a tumor suppressor gene, and its inhibition may promote tumor formation. In fact, this is not the case. The researchers have done a variety of experiments to prove that the anti-tumor effect of TM is achieved by inhibiting SIRT2 protein. Giannakakou said that it was the cooperation and exchange of ideas at the meeting, which led to its discovery related to c-Myc.
"Before this, we didn't have anything effective against cMyc protein. Most of the inhibitors were indirect, targeting other targets, and then lowering cMyc downstream. TM is also an indirect effect, but it shows both in vivo and in vitro. Very high activity. TM may further develop into clinical drugs."
The drawback of the TM that the team must deal with is its poor solubility and low bioavailability. Lin believes that by increasing solubility and bioavailability, they can further enhance the anti-tumor effect of TM.
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