Chapter 4
Summary and Conclusion
Peptide medicine has experienced nearly a hundred years of history from the earliest
application of bovine insulin to nowadays. Over the past century, with the continuous advancement of peptide synthesis methodology and purification methods, new
peptide molecules have entered the medical market one after another and several
of them have become blockbuster drugs for disease treatment. However, it should
not be ignored that most of these peptide molecules are obtained from natural products or modified products of natural molecules. There are very few examples of
artificially designed peptide molecules becoming drugs. With the continuous development of structural biology and systems biology, new drug targets are constantly
being revealed. To design effective ligands for these targets, small molecule shows
limitations. The emergence of new molecular modalities of drugs is continuing.
Peptides are considered to be the most effective molecular form for targeting nondruggable PPIs. Therefore, designing effective peptide drugs, enhancing the specificity of peptide molecules, improving the penetrating ability of peptide molecules,
and reducing the non-specific toxicity of peptide molecules are important goals for
the development of peptide drugs in the future.
This thesis focuses on the construction of stabilized helical peptides and creatively
proposed a novel chirality-induced helix system, from methodological development to structure-activity relationship research, and further develops protein-protein
interaction inhibitors based on this method to verifies the utility of the method.
To organize this thesis, I always focus on the most pressing issues in peptide
medicinal chemistry, trying to theoretically address some of the most fundamental
questions in the field of stabilized helical peptides, and put forward some basic
principles to instruct peptide drug design.
Chapter 1 introduces the importance of protein-protein interactions and the advantages of peptides in targeting protein-protein interactions. Moreover, a brief overview
of the current methodology for constructing helical peptides and the associated
limitations of them is performed.
© Springer Nature Singapore Pte Ltd. 2021
K. Hu, Development of In-Tether Carbon Chiral Center-Induced
Helical Peptide, Springer Theses,
https://doi.org/10.1007/978-981-33-6613-8_4
101
Summary and Conclusion
Peptide medicine has experienced nearly a hundred years of history from the earliest
application of bovine insulin to nowadays. Over the past century, with the continuous advancement of peptide synthesis methodology and purification methods, new
peptide molecules have entered the medical market one after another and several
of them have become blockbuster drugs for disease treatment. However, it should
not be ignored that most of these peptide molecules are obtained from natural products or modified products of natural molecules. There are very few examples of
artificially designed peptide molecules becoming drugs. With the continuous development of structural biology and systems biology, new drug targets are constantly
being revealed. To design effective ligands for these targets, small molecule shows
limitations. The emergence of new molecular modalities of drugs is continuing.
Peptides are considered to be the most effective molecular form for targeting nondruggable PPIs. Therefore, designing effective peptide drugs, enhancing the specificity of peptide molecules, improving the penetrating ability of peptide molecules,
and reducing the non-specific toxicity of peptide molecules are important goals for
the development of peptide drugs in the future.
This thesis focuses on the construction of stabilized helical peptides and creatively
proposed a novel chirality-induced helix system, from methodological development to structure-activity relationship research, and further develops protein-protein
interaction inhibitors based on this method to verifies the utility of the method.
To organize this thesis, I always focus on the most pressing issues in peptide
medicinal chemistry, trying to theoretically address some of the most fundamental
questions in the field of stabilized helical peptides, and put forward some basic
principles to instruct peptide drug design.
Chapter 1 introduces the importance of protein-protein interactions and the advantages of peptides in targeting protein-protein interactions. Moreover, a brief overview
of the current methodology for constructing helical peptides and the associated
limitations of them is performed.
© Springer Nature Singapore Pte Ltd. 2021
K. Hu, Development of In-Tether Carbon Chiral Center-Induced
Helical Peptide, Springer Theses,
https://doi.org/10.1007/978-981-33-6613-8_4
101