A team of researchers from Department of Chemistry and Biochemistry from Faculty of Science, University of Porto (FCUP) is working on a new drug to treat Parkinson's diseaseMore efficient and with fewer side effects than those currently used.
Parkinson's disease is a neurodegenerative disorder that results from the loss of nerve cells that produce an important neurotransmitter, dopamine, which is responsible for physiological processes such as cognition, memory, emotions, and movement control.
Drugs available on the market aim to increase dopamine production in the central nervous system. However, over the years, these drugs lose their effectiveness, making it necessary to give higher doses, which leads to side effects that in many cases may worsen the symptoms of the disease.
“Our goal is different: we focus on modulating dopamine receptors,” he begins to explain Ivo Dias, a researcher at the Associated Laboratory for Green Chemistry (LAQV-REQUIMTE) at FCUP who leads the research team. “What happens in Parkinson's disease is that low levels of dopamine are not sufficient to adequately activate the receptors, thus impairing the activation of dopamine circuits. What we want is to increase the affinity of these receptors for dopamine, thus ensuring relief of motor symptoms even at low concentrations of this neurotransmitter.”
In vitro improvement of a potential drug that exists naturally in our bodies
To this end, FCUP researchers are developing, in the laboratory, at scale Dina Pro Project, funded by the Science and Technology Foundation, analogues of the neuropeptide, melanostatin. Melanostatin, which was discovered in the 1970s, is naturally present in our bodies and is known for its anti-Parkinson's disease activity, which has already been proven in clinical trials. The goal is to improve its therapeutic potential, making it a drug candidate: with greater biological stability and improved gastrointestinal absorption.
“We discovered that one of the three amino acids that make up this substance can be modified at the structural level without damaging the modulating activity of dopamine receptors: proline,” the researcher describes.
Based on this modification, the FCUP team, within the scope of the DynaPro project, has already achieved promising results. In collaboration with partners from the University of Santiago de Compostela, they verified that the compounds developed in the laboratory are not only more efficient, but also do not cause toxicity in neurons. “We found that some of our analogues were more powerful than melanostatin, as they were able to activate receptors at a lower concentration than dopamine,” he says.
A pioneering therapeutic approach with promising results
With this new pharmacological approach, there is also an advantage in terms of side effects: “They are very low because melanostatin has no activity in the absence of dopamine.”
The FCUP team is one of the few in the world working on this therapeutic approach and is the only team in Portugal focusing on dopamine receptor modulators, which include melanostatin.
The DynaPro project ends later this year, and in light of the promising results, the researchers are preparing to file a patent application.
As next steps, they intend to conduct tests on the models In vivo To test the therapeutic potential of these compounds in different animal species.
This project is led by LAQV-REQUIMTE at FCUP and also includes researchers from the Faculty of Science and Technology of the University of the Basque Country and the Faculties of Pharmacy of the University of Porto (FFUP) and the University of Santiago de Compostela.
FCUP team is part of Ivo Dias that it Jose Enrique BorgesProfessors at FCUP, Integrated Researchers at LAQV-REQUIMTE, Researchers at LAQV-REQUIMTE, Sarah Reese, Hugo Almeida that it Beatriz Lima, PhD students in Sustainable Chemistry at FCUP that it xavier corea, Graduates From FCUP and also a researcher at this research center.
The project also includes the participation of researcher Vera Costa from FFUP, Professors Xerardo Mera from the University of Santiago de Compostela and Professors Humberto Diaz from the University of the Basque Country.
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