Abundant 'Secret Doors' on Human Proteins Could Reshape Drug Discovery
upstart writes:
Abundant 'secret doors' on human proteins could reshape drug discovery:
The number of potential therapeutic targets on the surfaces of human proteins is much greater than previously thought, according to the findings of a new study in the journal Nature.
A ground-breaking new technique developed by researchers at the Centre for Genomic Regulation (CRG) in Barcelona has revealed the existence of a multitude of previously secret doors that control protein function and which could, in theory, be targeted to dramatically change the course of conditions as varied as dementia, cancer and infectious diseases.
The method, in which tens of thousands of experiments are performed at the same time, has been used to chart the first ever map of these elusive targets, also known as allosteric sites, in two of the most common human proteins, revealing they are abundant and identifiable.
The approach could be a game changer for drug discovery, leading to safer, smarter and more effective medicines. It enables research labs around the world to find and exploit vulnerabilities in any protein-including those previously thought "undruggable."
"Not only are these potential therapeutic sites abundant, there is evidence they can be manipulated in many different ways. Rather than simply switching them on or off, we could modulate their activity like a thermostat. From an engineering perspective, that's striking gold because it gives us plenty of space to design 'smart drugs' that target the bad and spare the good," explains Andre Faure, postdoctoral researcher at the CRG and co-first author of the paper.
Journal Reference:
Faure, Andre J., Domingo, Julia, Schmiedel, Jorn M., et al. Mapping the energetic and allosteric landscapes of protein binding domains, Nature (DOI: 10.1038/s41586-022-04586-4)
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