Oral Peptides Revolutionize Drug Development: Game-Changer Alert!

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Prepare to be amazed! Finally, a breakthrough in drug development is here. Oral peptides, a cutting-edge innovation, are set to transform the treatment of diseases that have long resisted traditional oral medications. No more injections, no more inconvenience – these game-changing biologics can now target proteins with flat surfaces and specific homologs, all while being taken orally. Get ready for a new era in medicine!

Oral Peptides: A New Era in Drug Development

Introduction

Hey there, science enthusiasts! Today, we’re going to dive into an exciting breakthrough in drug development. Scientists have been working hard to find a way to make certain proteins more accessible for oral drug therapy. Traditionally, small molecules have struggled to bind to these proteins, and larger biologics have required injections, which can be inconvenient for patients. But now, researchers have made a significant discovery that could change the game!

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The Challenge

You see, there are many proteins that are crucial for treating various diseases, but they have remained elusive to oral drug therapy. These proteins have flat surfaces or require specificity for particular protein homologs, making it difficult for traditional small molecules to bind to them. And while larger biologics can target these proteins, they often require injections, which can be a hassle for patients.

The Breakthrough

In a recent study published in Nature Chemical Biology, scientists from the laboratory of Professor Christian Heinis at EPFL have achieved a major milestone in drug development. They have discovered a new class of orally available drugs that can address this long-standing challenge in the pharmaceutical industry. This is big news, folks!

The Focus: Cyclic Peptides

The researchers focused on a type of molecule called cyclic peptides. These molecules are known for their high affinity and specificity in binding challenging disease targets. However, developing cyclic peptides as oral drugs has proven difficult because they are rapidly digested or poorly absorbed by the gastrointestinal tract. But our brilliant scientists didn’t give up!

The Research Process

The research team targeted an enzyme called thrombin, which plays a critical role in blood coagulation. They wanted to find a way to develop cyclic peptides that could target thrombin and be stable enough to be taken orally. To do this, they used a two-step combinatorial synthesis strategy to create a vast library of cyclic peptides with thioether bonds, which enhance their stability when taken orally.

The “One Pot” Technique

The researchers developed a technique called the “one pot” method, where both steps of the synthesis process take place in the same reactive container. This eliminates the need for intermediate purification steps and allows for high-throughput screening directly in the synthesis plates. In simpler terms, they were able to create and test thousands of cyclic peptides at once!

The Results

Using this method, the researchers generated a comprehensive library of 8,448 cyclic peptides. These peptides showed a high affinity for thrombin and, when tested on rats, demonstrated oral bioavailability up to 18%. This means that when the cyclic peptide drug is taken orally, 18% of it successfully enters the bloodstream and has a therapeutic effect. This is a significant advancement for drugs in the biologics category!

The Future

By enabling the oral availability of cyclic peptides, the research team has opened up possibilities for treating a wide range of diseases that have been challenging to address with conventional oral drugs. They are now looking to target other disease targets, such as protein-protein interactions, and believe that even larger libraries of cyclic peptides can be synthesized and studied. The future looks promising!

Conclusion

So there you have it, folks! Oral peptides are paving the way for a new era in drug development. With this breakthrough, scientists are one step closer to making certain proteins more accessible for oral drug therapy, which will greatly benefit patients. The possibilities are endless, and we can’t wait to see what other discoveries lie ahead in the world of science and medicine. Stay curious and keep exploring!

SOURCE: Oral peptides: A new era in drug development

https://phys.org/news/2023-12-oral-peptides-era-drug.html

FAQ’s

1. What are cyclic peptides?

Cyclic peptides are a type of molecule known for their high affinity and specificity in binding challenging disease targets. They have a circular structure and are made up of amino acids.

2. How are cyclic peptides different from traditional small molecules and larger biologics?

Traditional small molecules have difficulty binding to certain proteins, while larger biologics often require injections. Cyclic peptides offer a potential solution by being able to target these proteins and being taken orally.

3. What is the significance of the “one pot” technique?

The “one pot” technique allows for the synthesis and testing of thousands of cyclic peptides simultaneously. This increases efficiency and enables high-throughput screening, leading to the discovery of potential drug candidates.

4. What is oral bioavailability?

Oral bioavailability refers to the percentage of a drug that enters the bloodstream and has a therapeutic effect when taken orally. In the case of the cyclic peptide drug, it was found to have an oral bioavailability of up to 18% in rats.

5. What are the future implications of this research?

By enabling the oral availability of cyclic peptides, this research opens up possibilities for treating diseases that have been challenging to address with conventional oral drugs. It also paves the way for the development of larger libraries of cyclic peptides and the targeting of other disease targets, such as protein-protein interactions.