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New Synthetic Compound Can Kill Superbugs’ Resistant to Antibiotics

by Universalwellnesssystems
myers research group

Researchers at Harvard University have developed an antibiotic that could overcome many drug-resistant infections that kill one million people each year and pose a global health threat.

A new synthetic compound called cresomycin has proven to be “highly effective” in killing deadly antibiotic-resistant superbugs such as Staphylococcus aureus and Pseudomonas aeruginosa.

Klesomycin is one of several promising compounds developed by a team at Harvard University to win the battle against superbugs.

A team led by Professor of Chemistry and Chemical Biology Andrew Myers reported in science How new molecules demonstrate an improved ability to bind to bacterial ribosomes, the biomolecular machines that control protein synthesis.

Disrupting ribosome function is a feature of many existing antibiotics, but some super-potent bacteria have evolved shielding mechanisms that prevent the drugs from working.

The new molecule is inspired by the chemical structure of lincosamides, a class of commonly prescribed antibiotics including clindamycin.

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Like many antibiotics, clindamycin is produced through semisynthesis, a process in which complex products isolated from nature are directly modified for pharmaceutical use. However, Harvard’s new compound is completely synthetic and features chemical modifications that are inaccessible by existing means.

“By harnessing the power of organic synthesis, the only limit when designing new antibiotics is your imagination,” said study co-author Ben Tresko. “Bacterial ribosomes are a favorite target for antimicrobial agents in nature, and these agents are the inspiration for our program.”

Bacteria develop antibiotics by expressing genes that produce enzymes (called ribosomal RNA methyltransferases) that remove drug components that are designed to attach to and destroy ribosomes, ultimately blocking the drug’s activity. You can acquire resistance to

To solve this problem, Dr. Myers and his team engineered the compound into a rigid shape that closely resembles its target, giving it a much stronger grip on ribosomes.

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The researchers describe the drug as “pre-tuned” for ribosome binding, as it does not need to expend as much energy to match its target as existing drugs.

The research team used component-based synthesis to identify cresomycin. This involves building large molecular components of equal complexity and integrating them at a later stage, a method pioneered by the Myers research group. This can be compared to the pre-build section before assembling a complex Lego set. .

This modular, complete synthesis system allows you to create and test not just one but hundreds of target molecules, significantly speeding up the drug discovery process.

“While we do not yet know whether klesomycin and its analogues are safe and effective in humans, our results demonstrate that compared to clinically approved antibiotics, they are effective against a long list of pathogenic bacterial strains. “This shows significantly improved inhibitory activity against In a Harvard University media release.

“Antibiotics form the foundation on which modern medicine is built,” co-author Kelvin Wu pointed out. “Without antibiotics, many cutting-edge medical procedures such as surgeries, cancer treatments, and organ transplants cannot be performed.”

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The research received early support from Harvard University’s Blavatnik Biomedical Accelerator, which awarded his lab funding in 2013 that allowed it to test drug compounds. Myers’ ongoing research also includes his recent award of a $1.2 million grant from a nonprofit organization to further develop oral antibiotics that could end the scourge of drug-resistant infections. Ta.

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