A new chemical technique discovered by researchers at the University of Leicester could unlock hyper-focused treatments for cancer and other diseases.
Illustration of a PROTAC. Credit: University of Leicester
An illustration of a PROTAC, the centre of this new technique. Credit: University of Leicester
The team used proteolysis - the process of breaking proteins down into amino acids - targeting chimeras (PROTACs) as a sort of bridge to aid in the degradation of proteins linked with cancer, which could allow for targeted applications of drugs and other treatments.
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In effect, this allows medical experts to manipulate the effectiveness of any cancer treatments by making changes to elements of this PROTAC bridge.
In medical terms, a "chimera" is anything, be it a person, organ, or tissue that contains cells with different genes than the rest of the person, organ or tissue.
The work, which was published in the Journal of Medicinal Chemistry, describes how the researchers applied this technique to degrade histone deacetylation enzymes (HDACs) with more precision than was previously possible.
The team states that HDACs play an important role in gene regulation, in which genes are switched 'on' or 'off', and are associated with a range of diseases, from cancer to Alzheimer's.
Using this method, treatment for diseases could allow for drugs to reach specific structures within a cancerous cell, opening the door for precision treatment.
Hyper-focusing drugs could also stand to increase potency in the required area while also lowering the rest of the body's exposure, which could limit potential side effects, the researchers state.
"We are really excited about what these new molecules are capable of in cancer cells and their potential future development in medicines", said Dr James Hodgkinson, an associate professor in organic chemistry at the university and one of the report's lead authors.
"Our next steps will involve optimising [targeted cells] chemical structure and biological properties so that one day they can be used to improve the lives of cancer patients".
The team have received a patent from the European Patent Office for the technique, which will now be fine-tuned.
The research has allowed the team to spearhead research that could lead to a vaccine for neurodegenerative disorders such as Alzheimer's.
"This work has been the result of a productive three-way collaboration between chemists, biologists and biophysicists - an exciting combination to deliver interdisciplinary research", said John Schwabe, a professor for structural biology at the University of Leicester and co-author of the study.
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"The potential of using specific degrades of therapeutic targets is very powerful".
- The following is a video explaining PROTACs and how they can be used to treat diseases:
Credit: University of Leicester
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