2019 Monash 3MT Winner - Beatrice Chiew, Pharmacy and Pharmaceutical Sciences
Summary
TLDRBeatrice 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.
Outlines
🧪 Chemical Space Exploration in Drug Discovery
Beatrice Shu from the Faculty of Pharmacy and Pharmaceutical Sciences introduces her project on improving drug discovery through efficient exploration of chemical space. She likens the vast number of potential therapeutic compounds to the stars in the sky, emphasizing the enormity of the task. The concept of chemical space, which is the range of possible chemical compounds, is explained, and the challenge of finding drugs that fit well with disease-causing proteins is highlighted. The speaker outlines the high costs and uncertain outcomes of drug discovery efforts, and introduces her project's aim to enhance the chances of discovering effective drugs by mapping chemical space more efficiently.
Mindmap
Keywords
💡Chemical Space
💡Drug Discovery
💡Structure Activity Relationships (SAR)
💡Protein Binding
💡Material Synthesis
💡Chemical Diversity
💡Off-Rate Screening
💡Breast Cancer
💡Drug Leads
💡Cost Efficiency
💡Kessel Run
Highlights
Speaker Beatrice Shu from the Faculty of Pharmacy and Pharmaceutical Sciences presents her project on improving drug discovery odds through efficient chemical space exploration.
The concept of 'chemical space' is introduced, representing the vast number of possible therapeutic compounds.
Only a small fraction of chemicals in chemical space fit well enough to proteins to be useful as drugs.
The high cost of drug discovery efforts, often yielding uncertain results, is highlighted.
The project aims to enhance the efficiency of navigating chemical space, likening it to making the Kessel run in under 12 parsecs.
Structure-activity relationships (SAR) are described as essential maps in the journey through chemical space.
SAR maps are costly to create, requiring the production and testing of numerous chemicals with purification being a bottleneck.
The first strategy involves designing large, structurally diverse chemical libraries that can be made in small volumes.
The second strategy allows for testing these chemical libraries without purification using off-rate screening.
Chemicals with a slower off-rate, indicating a better fit to proteins, can be identified as promising drug leads without purification.
Beatrice has applied these strategies to fight against breast cancer, making and testing over 600 chemicals in two years.
Three promising drug candidates have been identified through the project's innovative approach.
The potential to apply these strategies to more drug discovery programs could save billions of dollars.
The current statistics of drug discovery are challenged, with the project aiming to improve the odds of finding effective drugs.
The project's innovative methods and theoretical contributions are poised to have a significant impact on the field of drug discovery.
The practical application of the project's findings could lead to more efficient and cost-effective drug development.
Transcripts
[Music]
from the Faculty of Pharmacy and
Pharmaceutical Sciences is Beatrice Shu
and if there was ever someone who we
should have allowed to wear a costume
for their speech it is now because she
is looking at SAR Wars
a journey through chemical space how
many Thai fighters can we see up there
seven eight maybe how about stars
probably many more right well now let's
try and imagine all the possible
therapeutic compounds we could make say
we limit these to commonly found
elements in their realistic connections
that still tend to the 60 combinations
this is called chemical space and in
drug discovery that's a lot of space to
explore to be a drug a chemical must fit
well to a protein key to disease now in
the vast expanse of chemical space only
a tiny fraction of chemicals fit well
enough to proteins to be useful to us as
drugs which means billions of dollars
per year funneled into drug discovery
efforts which may or may not actually
yield a drug so with the odds of finding
a drug lower than Luc destroying the
Death Star you might be thinking I've
got a bad feeling about this and blame
you so my project aims at improving
these odds through efficient chemical
space exploration if drug discovery is
the Kessel run I want to make it in
under 12 parsecs now every journey needs
a map and in our journey through
chemical space these maps are called
structure activity relationships or SAR
and they relate the structure of a
chemical to changes in a protein but the
SAR Maps don't come cheap charting them
requires making and testing large
numbers of chemicals with purification
being the slowest step so we've come up
with two strategies to help fight in
these SAR wars the first involves
designing large libraries of
structurally diverse chemicals and
making them using material that would
fit in the volume of a tablespoon we can
explore huge areas of chemical space
using struck at were using chemical
diversity the second strategy allows us
to test these libraries without
purifying them we've learned that the
slower chemical leaves a pro
Jean measured by its off rate the better
it fits to that protein which makes
sense if you like something you're going
to stay around it much longer
now only chemicals that fit well to
proteins will have that slow off rate
impurities won't which means we can test
these large structurally diverse
libraries of chemicals without purifying
them using a technique called off rate
screening to rapidly identify the most
promising drug leads I've been using
these strategies to help fight against
breast cancer in just two years I've
been able to make and test over 600
chemicals build meaningful
structure-activity relationships and
have three promising candidates but the
sky is the limit if we can apply these
strategies to more drug discovery
programs who knows how many billions of
dollars we could save so so the current
statistics of drug discovery I say never
tell me the odds because we're punching
it in our journey through chemical space
[Music]
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