26 Result(s)

Article

Single-molecule FRET imaging of GPCR dimers in living cells

Class C G protein-coupled receptors (GPCRs) are known to form stable homodimers or heterodimers critical for function, but the oligomeric status of class A and B receptors, which constitute >90% of all GPCRs, ...

Wesley B. Asher, Peter Geggier, Michael D. Holsey, Grant T. Gilmore… in Nature Methods (2021)

Article

Activation of the GLP-1 receptor by a non-peptidic agonist

Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases, including diabetes and obesity¹. Structures of active receptors reveal peptide agonists engage deep within the receptor...

Peishen Zhao, Yi-Lynn Liang, Matthew J. Belousoff, Giuseppe Deganutti… in Nature (2020)

Article

Cryo-EM structure of the active, G_s-protein complexed, human CGRP receptor

Calcitonin gene-related peptide (CGRP) is a widely expressed neuropeptide that has a major role in sensory neurotransmission. The CGRP receptor is a heterodimer of the calcitonin receptor-like receptor (CLR) c...

Yi-Lynn Liang, Maryam Khoshouei, Giuseppe Deganutti, Alisa Glukhova… in Nature (2018)

Article

Crystal structure of the Frizzled 4 receptor in a ligand-free state

Frizzled receptors (FZDs) are class-F G-protein-coupled receptors (GPCRs) that function in Wnt signalling and are essential for develo** and adult organisms^1,2. As central mediators in this complex signalling p...

Shifan Yang, Yiran Wu, Ting-Hai Xu, Parker W. de Waal, Yuanzheng He, Mengchen Pu… in Nature (2018)

Article

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex

The structure of the glucagon-like peptide 1 receptor (GLP-1R) with its biased agonist exendin-P5 sheds light on both receptor activation and the mechanism of biased agonism.

Yi-Lynn Liang, Maryam Khoshouei, Alisa Glukhova, Sebastian G. B. Furness… in Nature (2018)

Reference Work Entry In depth

Secretin Receptor

Laurence J. Miller in Encyclopedia of Signaling Molecules (2018)

Reference Work Entry In depth

Cholecystokinin-1 Receptor

Laurence J. Miller in Encyclopedia of Signaling Molecules (2018)

Article

Phase-plate cryo-EM structure of a class B GPCR–G-protein complex

Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases, such as osteoporosis, diabetes and obesity. Here we report the structure of a full-length class B receptor, the calc...

Yi-Lynn Liang, Maryam Khoshouei, Mazdak Radjainia, Yan Zhang, Alisa Glukhova… in Nature (2017)

Living Reference Work Entry In depth

Secretin Receptor

Laurence J. Miller in Encyclopedia of Signaling Molecules

Living Reference Work Entry In depth

Cholecystokinin-1 Receptor

Laurence J. Miller in Encyclopedia of Signaling Molecules

Article

Membrane Cholesterol Affects Stimulus-Activity Coupling in Type 1, but not Type 2, CCK Receptors: Use of Cell Lines with Elevated Cholesterol

The lipid microenvironment of membrane proteins can affect their structure, function, and regulation. We recently described differential effects of acute modification of membrane cholesterol on the function of...

Kaleeckal G. Harikumar, Ross M. Potter, Achyut Patil, Valerie Echeveste… in Lipids (2013)

Article

Predicting the effects of amino acid replacements in peptide hormones on their binding affinities for class B GPCRs and application to the design of secretin receptor antagonists

Computational prediction of the effects of residue changes on peptide-protein binding affinities, followed by experimental testing of the top predicted binders, is an efficient strategy for the rational struct...

Jerez A. Te, Maoqing Dong, Laurence J. Miller… in Journal of Computer-Aided Molecular Design (2012)

Protocol

Use of Fluorescence Indicators in Receptor Ligands

Fluorescence techniques can provide insights into the environment of fluorescent indicators incorporated within a ligand as it is bound to its receptor. Fluorescent indicators of different sizes and chemical c...

Kaleeckal G. Harikumar, Laurence J. Miller in G Protein-Coupled Receptors in Drug Discovery (2009)

Protocol

Homology Modeling of GPCRs

Over 1000 sequences likely to encode G protein-coupled receptors (GPCRs) are currently available in publicly accessible and proprietary databases and this number may grow with the refinement of a number of dif...

John Simms, Nathan E. Hall, Polo H.C. Lam… in G Protein-Coupled Receptors in Drug Discov… (2009)

Protocol

Application of Fluorescence Resonance Energy Transfer Techniques to Establish Ligand–Receptor Orientation

Fluorescence resonance energy transfer (FRET) has been utilized to determine distances between a fluorescence donor and a fluorescence acceptor having appropriately overlap** spectra. In this chapter, we uti...

Kaleeckal G. Harikumar, Laurence J. Miller in G Protein-Coupled Receptors in Drug Discovery (2009)

Article

Exploration of the Endogenous Agonist Mechanism for Activation of Secretin and VPAC1 Receptors Using Synthetic Glycosylated Peptides

Current understanding of the molecular basis of activation of class II G protein-coupled receptors remains limited, despite recent solution of NMR and crystal structures of amino-terminal domains of several fa...

Maoqing Dong, Delia I. Pinon, Laurence J. Miller in Journal of Molecular Neuroscience (2008)

Article

Pattern of Intra-Family Hetero-Oligomerization Involving the G-Protein-Coupled Secretin Receptor

Oligomerization of G-protein-coupled receptors (GPCRs) is emerging as a mechanism for regulation and functional modification, although it has been studied most extensively for Family A receptors. Family B rece...

Kaleeckal G. Harikumar, Maria M. Morfis… in Journal of Molecular Neuroscience (2008)

Article

Fluorescence Characteristics of Hydrophobic Partial Agonist Probes of the Cholecystokinin Receptor

Fluorescence spectroscopic studies are powerful tools for the evaluation of receptor structure and the dynamic changes associated with receptor activation. Here, we have developed two chemically distinct fluor...

Kaleeckal G. Harikumar, Delia I. Pinon, Laurence J. Miller in Bioscience Reports (2006)