2019 Monash 3MT Winner - Beatrice Chiew, Pharmacy and Pharmaceutical Sciences

Summary

Beatrice Shu from the Faculty of Pharmacy and Pharmaceutical Sciences embarks on 'SAR Wars,' an innovative approach to drug discovery. She explores chemical space, the vast array of potential therapeutic compounds, and introduces two strategies to efficiently navigate it. Shu's project aims to enhance the odds of finding effective drugs by designing diverse chemical libraries and utilizing off-rate screening, a technique that identifies promising drug leads without the need for purification. Her work has already yielded three promising candidates for breast cancer treatment, showcasing the potential to save billions in drug discovery costs.

Takeaways

• 🎓 Beatrice Shu from the Faculty of Pharmacy and Pharmaceutical Sciences discusses her project on improving drug discovery through efficient chemical space exploration.
• 🌌 Chemical space refers to the vast number of possible therapeutic compounds, limited to commonly found elements and realistic connections, resulting in a large number of combinations.
• 💊 To be a drug, a chemical must fit well to a protein that is key to a disease, but only a tiny fraction of chemicals in chemical space meet this criterion.
• 💸 Drug discovery is an expensive process, with billions of dollars invested annually, but with no guarantee of yielding a successful drug.
• 🚀 Beatrice aims to improve the odds of finding useful drugs by making the process of exploring chemical space more efficient, likening it to the Kessel run in 'Star Wars'.
• 🗺️ Structure-activity relationships (SAR) are maps that relate the structure of a chemical to its effect on a protein, which are crucial for drug discovery but are costly to create.
• 🧪 The first strategy to combat SAR wars involves designing large libraries of structurally diverse chemicals that can be made in small volumes.
• 🔬 The second strategy is off-rate screening, a technique that allows testing of chemical libraries without purification by measuring how well chemicals fit to proteins based on their off-rate.
• 💡 Off-rate screening is significant because only chemicals that fit well to proteins will have a slow off-rate, allowing for the identification of promising drug leads without the need for purification.
• 🔑 Beatrice has applied these strategies to fight against breast cancer, making and testing over 600 chemicals and identifying three promising candidates within two years.
• 💰 The potential of these strategies could save billions of dollars if applied more broadly across drug discovery programs, improving the efficiency and cost-effectiveness of finding new drugs.

Q & A

What is the main topic of Beatrice Shu's speech?

The main topic of Beatrice Shu's speech is the exploration of chemical space in the context of drug discovery, focusing on improving the efficiency of finding therapeutic compounds.

What is meant by 'chemical space' in the context of drug discovery?

In drug discovery, 'chemical space' refers to the vast number of possible therapeutic compounds that could theoretically be made, limited to commonly found elements and realistic connections.

Why is it challenging to find drugs within the chemical space?

Finding drugs within the chemical space is challenging because only a tiny fraction of chemicals fit well enough to proteins to be useful as drugs, and the exploration of this space requires significant investment and resources.

What is the significance of structure-activity relationships (SAR) in drug discovery?

Structure-activity relationships (SAR) are significant in drug discovery as they relate the structure of a chemical to changes in a protein, which helps in understanding how different compounds interact with biological targets.

What are the two strategies Beatrice Shu's project employs to improve chemical space exploration?

The two strategies are: 1) Designing large libraries of structurally diverse chemicals and making them in small volumes, and 2) Testing these libraries without purifying them using a technique called off-rate screening.

How does the off-rate screening technique work in identifying promising drug leads?

Off-rate screening works by measuring how quickly a chemical dissociates from a protein. Chemicals that fit well to proteins have a slower off-rate, indicating a stronger interaction, which is desirable for drug candidates.

What is the goal of Beatrice Shu's project in terms of improving drug discovery efficiency?

The goal of Beatrice Shu's project is to make the process of drug discovery more efficient by reducing the time and resources needed to explore chemical space and identify promising drug candidates.

How many chemicals has Beatrice Shu made and tested in her project against breast cancer?

Beatrice Shu has made and tested over 600 chemicals in her project against breast cancer.

What are the potential benefits of applying these strategies to more drug discovery programs?

Applying these strategies to more drug discovery programs could potentially save billions of dollars and increase the chances of finding effective drugs.

What is the current state of drug discovery according to the speaker?

According to the speaker, the current state of drug discovery is challenging, with low odds of finding a successful drug, but the speaker is optimistic about improving these odds through innovative strategies.

What is the metaphor used by Beatrice Shu to describe the difficulty of finding a drug in chemical space?

Beatrice Shu uses the metaphor of the Kessel run from Star Wars to describe the difficulty of finding a drug in chemical space, likening it to making the Kessel run in under 12 parsecs.