GPCR Cryo-EM and Drug Design

Unlocking GPCR structure based drug design

"High-resolution structures will play an important role in creation of better medicines—medicines that could potentially be personalized to a patient, that target unmet medical need and reduce side-effects."

                                                        -Prof. Patrick Sexton                 

Background

Working within the Monash University Institute of Pharmaceutical Science, Prof. Patrick Sexton’s team is uncovering the secrets of the largest family of cell surface receptors, G protein-coupled receptors (GPCRs). These receptors allow communication between external signals and the inside of cells. GPCRs are the most intensely studied class of drug targets, accounting for approximately 35% of approved drugs. However, GPCRs are highly challenging membrane proteins. They are difficult to produce and have proven to be equally difficult for structural characterization. In general, drugging of GPCRs is chemically driven (i.e., without the use of structures), but cryo-EM (cryo-electron microscopy) is showing great promise in unlocking GPCR structure-based drug design.

Prof. Patrick Sexton

Collaboration

Prof. Patrick Sexton and his team are luminaries in GPCR research, particularly cryo-EM of GPCRs, including production of novel highly challenging GPCR complexes. Based on the advances uncovered by his laboratory’s research, Prof. Sexton has established collaborations with several pharmaceutical companies. Now, he has entered into a collaboration with Thermo Fisher Scientific to progress GPCR Cryo-EM and Drug Design. This collaboration is a joint effort dedicated to bringing cryo-EM of GPCRs closer to industry scientists.

The GPCR Cryo-EM and Drug Design program utilizes a Thermo Scientific Glacios Cryo-TEM facility as a key component of the workflow that is linked to imaging on Thermo Scientific Krios Cryo-TEM data collection facilities on the Monash University campus or via collaborations.

Workshops and partnering

Cryo-EM is opening up unprecedented opportunities for structure-based drug discovery on GPCRs. The GPCR Cryo-EM and Drug Design collaboration encompasses the spectrum of GPCR cryo-EM competence, from protein production, specimen preparation, and grid screening to data collection and reconstruction. A key goal of the collaboration is to make cryo-EM of GPCRs easier for all, particularly industry, by offering workshops and (short-term) placements for industry.

Cryo-EM is highly productive for solving the structures of GPCRs, and the technology is readily transferred. New sub-3 Å cryo-EM structures of high-value GPCRs are routinely determined in Prof. Sexton’s laboratory. Workshops will focus on key aspects of the GPCR cryo-EM workflow.

GPCRs in a new light

Prof. Sexton's team is also at the forefront of unravelling novel aspects of GPCR pharmacology. Want to learn more about his lab’s groundbreaking work on GPCRs? Read more ›

Download White Paper

Learn from our collaborators how to prepare ideal GPCR cryo-EM specimen. This robust workflow delivers a high success rate for achieving sub-2.5A reconstructions of GPCRs.

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Registration

When you sign up, you will be the first to learn about upcoming GPCR Cryo-EM and Drug Design workshops and placements, and you will receive information on opportunities for industry engagement.

 

 

 

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