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Carbohydrates, known as the third major class of biological macromolecules after proteins and nucleic acids, have been found to be actively involved in numerous aspects of lives, such as providing the energy source for cell proliferation, supporting the structure of organisms, constituting invasion and host defense systems, and forming antibiotics secondary metabolites. Carbohydrates and their derivatives have been widely explored as therapeutic agents for treating viral infections, bacterial infections, cancer, diabetes, cardiovascular diseases, nervous system disorders, etc. During 2000 to 2021, a total of 54 drugs or diagnostic agents containing carbohydrate moieties as the major structural units have been approved.

Rational structural design and chemical synthesis plays vital roles in the development of carbohydrate-based drugs. For example, chemical glycosylation reaction is the key step during the synthesis of blockbuster drugs Empagliflozin and Dapagliflozin, both of which are glycoconjugate SGLT2 inhibitors for treating type 2 diabetes. Glycopeptides are emerging as promising biochemical probes and therapeutic agents, the synthesis of which usually requires site-specific glycosylation of amino acid residues. Via utilizing the Warburg effect, numerous glycoconjugates have been designed and synthesized for targeted cancer therapy using carbohydrate moieties as cancer-targeting warheads. Particularly, some glycoconjugates act as prodrugs that are activated in tumor microenvironment to release the parental drugs. Another important field of carbohydrate-based drug development focuses on employing glycol-nanocarriers as drug delivery systems for treating a variety of diseases.

The focus of this Research Topic of Frontiers in Chemistry is to highlight recent advancements in carbohydrate-based drug research and development. Areas to be covered in this Research Topic may include, but are not limited to:
• Glycoconjugate drugs for treating various diseases;
• Carbohydrate-based prodrugs for spatial/temporal-controlled drug release;
• Chemical methods in synthesizing carbohydrate-based bioactive molecules;
• Glycopeptides and their biological applications;
• Glycol-nanocarriers as novel drug delivery systems.

Keywords: glycoconjugate, glycol-nanocarriers, carbohydrate-based drugs, structural design, chemical synthesis


Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.

Carbohydrates, known as the third major class of biological macromolecules after proteins and nucleic acids, have been found to be actively involved in numerous aspects of lives, such as providing the energy source for cell proliferation, supporting the structure of organisms, constituting invasion and host defense systems, and forming antibiotics secondary metabolites. Carbohydrates and their derivatives have been widely explored as therapeutic agents for treating viral infections, bacterial infections, cancer, diabetes, cardiovascular diseases, nervous system disorders, etc. During 2000 to 2021, a total of 54 drugs or diagnostic agents containing carbohydrate moieties as the major structural units have been approved.

Rational structural design and chemical synthesis plays vital roles in the development of carbohydrate-based drugs. For example, chemical glycosylation reaction is the key step during the synthesis of blockbuster drugs Empagliflozin and Dapagliflozin, both of which are glycoconjugate SGLT2 inhibitors for treating type 2 diabetes. Glycopeptides are emerging as promising biochemical probes and therapeutic agents, the synthesis of which usually requires site-specific glycosylation of amino acid residues. Via utilizing the Warburg effect, numerous glycoconjugates have been designed and synthesized for targeted cancer therapy using carbohydrate moieties as cancer-targeting warheads. Particularly, some glycoconjugates act as prodrugs that are activated in tumor microenvironment to release the parental drugs. Another important field of carbohydrate-based drug development focuses on employing glycol-nanocarriers as drug delivery systems for treating a variety of diseases.

The focus of this Research Topic of Frontiers in Chemistry is to highlight recent advancements in carbohydrate-based drug research and development. Areas to be covered in this Research Topic may include, but are not limited to:
• Glycoconjugate drugs for treating various diseases;
• Carbohydrate-based prodrugs for spatial/temporal-controlled drug release;
• Chemical methods in synthesizing carbohydrate-based bioactive molecules;
• Glycopeptides and their biological applications;
• Glycol-nanocarriers as novel drug delivery systems.

Keywords: glycoconjugate, glycol-nanocarriers, carbohydrate-based drugs, structural design, chemical synthesis


Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.

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