F1000 recommendation of The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

Press/Media: Expert Comment

Description

Commentary on:

 

Wootten D, Reynolds CA, Smith KJ, Mobarec JC, Koole C, Savage EE, Pabreja K, Simms J, Sridhar R, Furness SGB, Liu M, Thompson PE, Miller LJ, Christopoulos A, Sexton PM. The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism. Cell. 2016 Jun 16;165(7):1632-1643. doi: 10.1016/j.cell.2016.05.023. PubMed PMID: 27315480; PubMed Central PMCID: PMC4912689.

Period16 Jun 2016

Media contributions

1

Media contributions

  • TitleF1000 recommendation
    Degree of recognitionInternational
    Media name/outletF1000
    Media typeWeb
    Date16/06/16
    Descriptionhis is an exceptionally thorough study, which combines site-directed mutagenesis, molecular modeling, in vitro signaling and molecular dynamics studies to arrive at a three-dimensional representation of key residues implicated in biased agonism at the GLP-1 (glucagon-like peptide 1) receptor. As GLP-1 agonists continue to represent therapeutics for a variety of metabolic disorders, understanding the molecular and eventually atomic mechanisms for biased signaling and functional selectivity at this receptor has important theoretical and therapeutic implications.

    Going forward, it will be important to correlate these findings with direct biophysical and structural studies of GLP-1R.

    Disclosures
    None declared

    Roth B: F1000Prime Recommendation of [Wootten D et al., Cell 2016 165(7):1632-1643]. In F1000Prime, 11 Oct 2016; 10.3410/f.726430827.793523956
    Producer/AuthorBrian Roth
    URLhttps://f1000.com/prime/726430827
    PersonsSebastian Furness