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HRI has developed an unprecedented drug design strategy that tailors drugs with fatty acids to minimise side effects.

Drugs targeting kinase – a critical class of enzymes that mediate all aspects of human physiology and pathology – are a rising star among new drug candidates for treating cardiovascular disease and cancer, due to their effectiveness and rapid response. However, their associated side effects are a huge barrier to further development for clinical use.

Dr Xuyu Liu, leader of the Cardiovascular-protective Signalling and Drug Discovery Group at HRI, has developed an approach that effectively minimises the side effects of kinase drugs.

“Kinase drugs have enormous potential for effectively treating cardiovascular disease, but their associated side effects can outweigh their treatment benefits,” says Dr Liu.

We have devel­oped an unprece­dent­ed approach to fur­ther the activ­i­ty of kinase drugs and make them safer and suit­able to use for car­dio­vas­cu­lar treatment.”

“Currently, our research is focusing on elaborating this technology as a generic strategy to optimise kinase drugs for cardiovascular disease.”

In this approach, the Group discovered that certain fatty acids display a high toxicity toward breast cancers by targeting mis-regulated Akt kinases, which also promote the health of the cardiovascular system and boost the immune system in normal physiological circumstances. Following this logic, the Group tailored an existing Phase II kinase drug to resemble the action of these fatty acids to increase potency. Importantly, these new drug candidates do not trigger serious side effects associated with other trialled Akt drugs, such as diabetes-like syndrome, metabolic mis-regulation and an irritation response.

One of Dr Liu’s new drug candidates proved in pre-clinical trials to be superior to the original drug, with an excellent safety profile that is suitable for application in cardiovascular disease and diabetes treatment. Evidence from lab models suggests that this drug could be an exciting candidate for the treatment of factors in cardiovascular disease such as thrombosis (blood clots) and pathological cardiac hypertrophy.

The Group is currently conducting further research to repurpose this drug as a candidate for antithrombotic, cardioprotective and diabetic therapies.

“This strategy can be further developed as a generic platform to increase the safety profiles of other cardiovascular and anticancer drugs,” states Dr Liu.

Hav­ing safer and more effec­tive treat­ment options would have a huge impact on the mil­lions of peo­ple suf­fer­ing from car­dio­vas­cu­lar dis­ease, and can­cer, around the world.”


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