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This article is original by Translational Medicine Network.
Please indicate the source for reprinting.
Author: chen Introduction: Recently, scientists at the University of Cambridge in the UK have taken a promising step in developing new drugs for the treatment of acute myeloid leukemia! For the first time, they used enzymes that play an important role in protein expression as targets for fighting cancer.
Acute myelogenous leukemia (AML) is a cancer of the hematopoietic system caused by abnormal proliferation of bone marrow white blood cells (not lymphoid white blood cells).
Once the disease occurs, people usually need months of intensive chemotherapy and long-term hospitalization, and the incidence increases with age.
In the UK, approximately 3100 people are diagnosed with this disease every year, most of whom are over 65 years old.
The mainstream treatment of AML on the market has not changed much for decades, and less than one-third of people can survive from it.
Previously, in order to determine a potential new method for the treatment of AML, researchers have discovered that an enzyme called METTL3 plays a key role in the occurrence and development of AML.
When METL3 is inhibited, no methyl group is added to the RNA, which prevents the production of its essential protein, so AML cells begin to die.
However, there is currently a lack of research on small molecule drugs that can specifically inhibit METTL3 to treat AML.
On April 26, 2021, researchers from the University of Cambridge in the United Kingdom reported a new method for the treatment of AML, and published the research results in "Nature" entitled "Small molecule inhibition of METTL3 as a strategy against myeloid leukaemia".
They found that STM2457 is a specific inhibitor of METTL3 enzyme.
Inhibition of METTL3 by the small drug molecule STM2457 can block the carcinogenesis caused by the overexpression of enzymes, thereby significantly inhibiting the process of AML.
Our genetic code is written in DNA, but in order to produce proteins (molecules vital to the function of organisms), we first need to convert DNA into RNA.
The production of protein is controlled by enzymes, and enzymes produce chemical changes to RNA.
Sometimes, these enzymes are improperly regulated and produce too much protein.
In order to screen for effective METTL3 inhibitors, the researchers conducted high-throughput screening of 250,000 drug-like compounds, and they found that STM2457 has a better inhibitory effect.
Then the researchers conducted structural analysis and enzyme activity experiments, and concluded that STM2457 can inhibit the activity of the methyltransferase of METL3 by binding to the SAM (S-adenosyl methionine) binding site of METL3, that is, STM2457.
It is a specific inhibitor of METTL3.
In order to study the anti-AML potential of STM2457, the researchers conducted in vitro cell experiments.
The results showed that STM2457 significantly reduced the growth and proliferation of cell lines from AML patients, and induced apoptosis to kill cancer cells.
Then, the researchers transplanted cells from AML patients into immunocompromised mice to simulate the disease (mouse model) (picture).
When they treated mice with STM2457, they found that it could hinder the proliferation and expansion of transplanted cells, reduce the number of leukemia cells in the bone marrow and spleen of the mice, and significantly extend the life of the mice, and the drug has no toxic side effects.
.
Figure STM2457's effect on leukemia mice.
In short, STM2457 is a specific inhibitor of METTL3, which can block the carcinogenesis caused by the overexpression of the enzyme.
At the same time, this research for the first time used enzymes that play an important role in the protein expression process as targets against cancer, providing new ideas for the development of cancer drugs, or marking the beginning of a new era of cancer treatment.
The researchers said: "Protein is essential to our body functions, and its production process involves the conversion of DNA to RNA.
Sometimes, the process may go wrong and may have devastating consequences for human health.
So far, no one has found that This indispensable process, a treatment method aimed at fighting cancer, is the beginning of a new era of cancer treatment.
"Reference:: This article aims to introduce the progress of medical research and cannot be used as a reference for treatment options.
If you need health guidance, please go to a regular hospital for treatment.
Please indicate the source for reprinting.
Author: chen Introduction: Recently, scientists at the University of Cambridge in the UK have taken a promising step in developing new drugs for the treatment of acute myeloid leukemia! For the first time, they used enzymes that play an important role in protein expression as targets for fighting cancer.
Acute myelogenous leukemia (AML) is a cancer of the hematopoietic system caused by abnormal proliferation of bone marrow white blood cells (not lymphoid white blood cells).
Once the disease occurs, people usually need months of intensive chemotherapy and long-term hospitalization, and the incidence increases with age.
In the UK, approximately 3100 people are diagnosed with this disease every year, most of whom are over 65 years old.
The mainstream treatment of AML on the market has not changed much for decades, and less than one-third of people can survive from it.
Previously, in order to determine a potential new method for the treatment of AML, researchers have discovered that an enzyme called METTL3 plays a key role in the occurrence and development of AML.
When METL3 is inhibited, no methyl group is added to the RNA, which prevents the production of its essential protein, so AML cells begin to die.
However, there is currently a lack of research on small molecule drugs that can specifically inhibit METTL3 to treat AML.
On April 26, 2021, researchers from the University of Cambridge in the United Kingdom reported a new method for the treatment of AML, and published the research results in "Nature" entitled "Small molecule inhibition of METTL3 as a strategy against myeloid leukaemia".
They found that STM2457 is a specific inhibitor of METTL3 enzyme.
Inhibition of METTL3 by the small drug molecule STM2457 can block the carcinogenesis caused by the overexpression of enzymes, thereby significantly inhibiting the process of AML.
Our genetic code is written in DNA, but in order to produce proteins (molecules vital to the function of organisms), we first need to convert DNA into RNA.
The production of protein is controlled by enzymes, and enzymes produce chemical changes to RNA.
Sometimes, these enzymes are improperly regulated and produce too much protein.
In order to screen for effective METTL3 inhibitors, the researchers conducted high-throughput screening of 250,000 drug-like compounds, and they found that STM2457 has a better inhibitory effect.
Then the researchers conducted structural analysis and enzyme activity experiments, and concluded that STM2457 can inhibit the activity of the methyltransferase of METL3 by binding to the SAM (S-adenosyl methionine) binding site of METL3, that is, STM2457.
It is a specific inhibitor of METTL3.
In order to study the anti-AML potential of STM2457, the researchers conducted in vitro cell experiments.
The results showed that STM2457 significantly reduced the growth and proliferation of cell lines from AML patients, and induced apoptosis to kill cancer cells.
Then, the researchers transplanted cells from AML patients into immunocompromised mice to simulate the disease (mouse model) (picture).
When they treated mice with STM2457, they found that it could hinder the proliferation and expansion of transplanted cells, reduce the number of leukemia cells in the bone marrow and spleen of the mice, and significantly extend the life of the mice, and the drug has no toxic side effects.
.
Figure STM2457's effect on leukemia mice.
In short, STM2457 is a specific inhibitor of METTL3, which can block the carcinogenesis caused by the overexpression of the enzyme.
At the same time, this research for the first time used enzymes that play an important role in the protein expression process as targets against cancer, providing new ideas for the development of cancer drugs, or marking the beginning of a new era of cancer treatment.
The researchers said: "Protein is essential to our body functions, and its production process involves the conversion of DNA to RNA.
Sometimes, the process may go wrong and may have devastating consequences for human health.
So far, no one has found that This indispensable process, a treatment method aimed at fighting cancer, is the beginning of a new era of cancer treatment.
"Reference:: This article aims to introduce the progress of medical research and cannot be used as a reference for treatment options.
If you need health guidance, please go to a regular hospital for treatment.
