For decades, a significant number of proteins that are crucial for treating various diseases have remained difficult to target with oral drug therapy. Traditional small molecules often struggle to bind to proteins with flat surfaces or require specificity for specific protein homologs. Typically, larger biologics that can target these proteins require injection, which limits patient convenience and accessibility.
“There are numerous diseases in which the targets have been identified, but drugs that can bind to and reach them have not been developed,” says Heinis. “Most of these diseases are types of cancer, and many targets in these cancers are protein-protein interactions that are essential for tumor growth but cannot be inhibited.”
The study focused on cyclic peptides, which are versatile molecules known for their high affinity and specificity in binding challenging disease targets. However, developing cyclic peptides as oral drugs has proven to be difficult because they are rapidly digested or poorly absorbed by the gastrointestinal tract.
“Cyclic peptides are highly promising for drug development as they can bind to challenging targets for which it has been difficult to generate drugs using established methods,” says Heinis. “However, cyclic peptides are typically not suitable for oral administration as a pill, which greatly limits their application.”
The research team targeted the enzyme thrombin, which is a critical disease target due to its central role in blood coagulation. Regulating thrombin is crucial for preventing and treating thrombotic disorders such as strokes and heart attacks.
2023-12-28 21:00:04
Post from phys.org rnrn
