ArticleAngewandte Chemie (International ed. in English)2014
Peptide modifications differentially alter G protein-coupled receptor internalization and signaling bias.
Article in Angewandte Chemie (International ed. in English), 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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Who cites it
14 citing papers in PubMed, 40 citations in OpenAlex.
- The pathway-independent positive allosteric modulator C1 allows for the identification of active YCellular and molecular life sciences : CMLS · 2026Article
- Potent and Protease Resistant Azapeptide Agonists of the GLP-1 and GIP Receptors.Angewandte Chemie (International ed. in English) · 2024Article
- Article
- A Non-Perturbative Molecular Grafting Strategy for Stable and Potent Therapeutic Peptide Ligands.ACS central science · 2021Article
- Biased agonists at the human YCellular and molecular life sciences : CMLS · 2020Article
- Labeling a TCO-functionalized single domain antibody fragment withBioorganic & medicinal chemistry · 2020Article
- Design, synthesis, and biological evaluation of a multifunctional neuropeptide-Y conjugate for selective nuclear delivery of radiolanthanides.EJNMMI research · 2020Article
- The Fascinating Chemistry of α-Haloamides.ChemistryOpen · 2020Review
- NPYMolecular metabolism · 2020Article
- Chemical Strategies for Half-Life Extension of Biopharmaceuticals: Lipidation and Its Alternatives.ACS medicinal chemistry letters · 2018Article
- C-terminal motif of human neuropeptide YCellular signalling · 2017Article
- High molecular weight PEGylation of human pancreatic polypeptide at position 22 improves stability and reduces food intake in mice.British journal of pharmacology · 2016Article
- Pancreatic polypeptide and its central Y4 receptors are essential for cued fear extinction and permanent suppression of fear.British journal of pharmacology · 2016Article
- Position and length of fatty acids strongly affect receptor selectivity pattern of human pancreatic polypeptide analogues.ChemMedChem · 2014Article
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 3 countries.
Funding
Abstract
Although G protein-coupled receptors (GPCRs) are targeted by more clinically used drugs than any other type of protein, their ligand development is particularly challenging. Humans have four neuropeptide Y receptors: hY1R and hY5R are orexigenic, while hY2R and hY4R are anorexigenic, and represent important anti-obesity drug targets. We show for the first time that PEGylation and lipidation, chemical modifications that prolong the plasma half-lives of peptides, confer additional benefits. Both modifications enhance pancreatic polypeptide preference for hY2R/hY4R over hY1R/hY5R. Lipidation biases the ligand towards arrestin recruitment and internalization, whereas PEGylation confers the opposite bias. These effects were independent of the cell system and modified residue. We thus provide novel insights into the mode of action of peptide modifications and open innovative venues for generating peptide agonists with extended therapeutic potential.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.