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Scientists from Heptares Therapeutics have used Diamond Light Source, the UK’s national synchrotron facility, to understand the structure of a protein involved in Parkinson’s disease and other neurological disorders. Their findings, published this week in the journal Structure, could pave the way for a new generation of targeted drug treatments.
The team used Diamond’s Microfocus Macromolecular Crystallography (MX) beamline (I24) to reveal the complex structure of the vital adenosine A2A receptor and show how xanthine-based drugs such as caffeine bind to their target. Adenosine A2A receptors regulate the effects of neurotransmitters in the brain, cardiovascular and immune systems, and are of particular interest as a drug target for Parkinson’s disease. Although it was known that caffeine inhibits the action of the adenosine, the exact molecular mechanism involved was not fully understood.
“These co-structures of xanthines in complex with the adenosine A2A receptor advance our understanding of what is happening at the molecular level when the drug binds to its target and blocks the receptor’s response. Along with novel chemotypes discovered by our team, the structural data we collected at Diamond is enabling us to develop highly optimised next-generation drug candidates for Parkinson’s disease and other neurological disorders,” said Dr. Fiona Marshall, Chief Scientific Officer at Heptares.
phys.org
The team used Diamond’s Microfocus Macromolecular Crystallography (MX) beamline (I24) to reveal the complex structure of the vital adenosine A2A receptor and show how xanthine-based drugs such as caffeine bind to their target. Adenosine A2A receptors regulate the effects of neurotransmitters in the brain, cardiovascular and immune systems, and are of particular interest as a drug target for Parkinson’s disease. Although it was known that caffeine inhibits the action of the adenosine, the exact molecular mechanism involved was not fully understood.
“These co-structures of xanthines in complex with the adenosine A2A receptor advance our understanding of what is happening at the molecular level when the drug binds to its target and blocks the receptor’s response. Along with novel chemotypes discovered by our team, the structural data we collected at Diamond is enabling us to develop highly optimised next-generation drug candidates for Parkinson’s disease and other neurological disorders,” said Dr. Fiona Marshall, Chief Scientific Officer at Heptares.
Coffee could offer key ingredient for new treatments for Parkinson's disease
Scientists from Heptares Therapeutics have used Diamond Light Source, the UK’s national synchrotron facility, to understand the structure of a protein involved in Parkinson’s disease and other neurological disorders. Their findings, published this week in the journal Structure, could pave the...
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