AI Article Synopsis
- - G protein-coupled receptors (GPCRs) are the largest family of membrane proteins and are key targets for drug development, especially class A GPCRs, which affect many physiological processes in humans.
- - About 45% of GPCRs bind flexible peptides or segments from larger protein ligands, with existing research indicating these peptides can change shape significantly when bound to receptors.
- - To improve knowledge on how these peptides interact with receptors and inform peptidomimetic drug design, more research is needed on peptide ligands in their complexed state with the corresponding GPCRs.
Article Abstract
G protein-coupled receptors (GPCRs) represent the largest membrane protein family and a significant target class for therapeutics. Receptors from GPCRs' largest class, class A, influence virtually every aspect of human physiology. About 45% of the members of this family endogenously bind flexible peptides or peptides segments within larger protein ligands. While many of these peptides have been structurally characterized in their solution state, the few studies of peptides in their receptor-bound state suggest that these peptides interact with a shared set of residues and undergo significant conformational changes. For the purpose of understanding binding dynamics and the development of peptidomimetic drug compounds, further studies should investigate the peptide ligands that are complexed to their cognate receptor.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8746363 | PMC |
| http://dx.doi.org/10.3390/molecules27010210 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!