Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors
| Autor: | John A. Christopher, Giles A. Brown, Miles Congreve, Rie Suzuki, Conor C. G. Scully |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
endocrine system
Peptide Computational biology 01 natural sciences Dipeptidyl peptidase Glucagon-Like Peptide-1 Receptor 03 medical and health sciences Glucagon-Like Peptide 1 Drug Discovery Glucagon-Like Peptide 2 Animals Humans Hypoglycemic Agents Amino Acid Sequence Peptide sequence 030304 developmental biology chemistry.chemical_classification 0303 health sciences Drug discovery digestive oral and skin physiology Rational design Proglucagon Glucagon-like peptide-1 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry Drug Design Glucagon-Like Peptide-2 Receptor Molecular Medicine Anti-Obesity Agents Peptides Glucagon receptor hormones hormone substitutes and hormone antagonists |
| Zdroj: | Journal of medicinal chemistry. 63(3) |
| ISSN: | 1520-4804 |
| Popis: | Glucagon-like peptide 1 (GLP-1) and glucagon-like peptide 2 (GLP-2) are proglucagon derived peptides that are released from gut endocrine cells in response to nutrient intake. These molecules are rapidly inactivated by the action of dipeptidyl peptidase IV (DPP-4) which limits their use as therapeutic agents. The recent emergence of three-dimensional structures of GPCRs such as GLP-1R and glucagon receptor has helped to drive the rational design of innovative peptide molecules that hold promise as novel peptide therapeutics. One emerging area is the discovery of multifunctional molecules that act at two or more pharmacological systems to enhance therapeutic efficacy. In addition, drug discovery efforts are also focusing on strategies to improve patient convenience through alternative routes of peptide delivery. These novel strategies highlight the broad utility of peptide-based therapeutics in human disease settings where unmet needs still exist. |
| Databáze: | OpenAIRE |
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