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Optimising Targeted Protein Degradation

02MedChemNet and Future Medicinal Chemistry editors Jasmine Harris and Ben Walden interviewed George Burslem from Yale University at the Global Medicinal Chemistry and GPCR Summit.

Can you please introduce yourself and tell us about your institution?

My name’s George Burslem. I’m a chemical biologist and at the moment I’m working in Crews Lab at Yale University. I work on several projects, mostly around targeted protein degradation and the development of proteolysis targeting chimeras (PROTACs). Most recently I’ve been working on targeted protein degradation of receptor tyrosine kinases (RTKs) to show that this PROTAC technology is capable of degrading transmembrane proteins.

Could you give us a summary of the talk you delivered at the Global Medicinal Chemistry and GPCR Summit?

I spoke about the recent work that we have recently published on understanding the role of protein-protein interactions in the development of successful PROTACs, as well as showing the advantages of degradation over inhibition, particularly in the cases of RTKs.

I think that we will continue to develop PROTAC technology against new targets and continue to understand the ways in which we can optimise targeted protein degradation. Hopefully we’ll be able to progress this into benefiting patients by understanding the role of structural scaffolding functions of proteins, which could potentially be targeted in a way that is not available through traditional small molecule inhibition.

Do you think this will have a big impact in the future of drug development?

I think that certainly PROTACs have the potential to function in ways that traditional small molecules can’t. Removing scaffolding roles rather than just inhibiting enzymatic activity is something that we are really interested in with respect to PROTAC development.

 

George Burslem is a Research Fellow in the Crews Lab at Yale University.

 

The next Medicinal Chemistry Summit will take place September 17 – 18 in Boston. Take a look at the agenda.

 

Medicinal Chemistry Summit: USA

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