Critical features for biosynthesis, stability, and functionality of a G protein-coupled receptor uncovered by all-versus-all mutations

KM Schlinkmann, A Honegger… - Proceedings of the …, 2012 - National Acad Sciences
The structural features determining efficient biosynthesis, stability in the membrane and,
after solubilization, in detergents are not well understood for integral membrane proteins …

Stabilization of G protein-coupled receptors by point mutations

FM Heydenreich, Z Vuckovic, M Matkovic… - Frontiers in …, 2015 - frontiersin.org
G protein-coupled receptors (GPCRs) are flexible integral membrane proteins involved in
transmembrane signaling. Their involvement in many physiological processes makes them …

Maximizing detergent stability and functional expression of a GPCR by exhaustive recombination and evolution

KM Schlinkmann, M Hillenbrand, A Rittner… - Journal of molecular …, 2012 - Elsevier
To identify structural features in a G‐protein‐coupled receptor (GPCR) crucial for
biosynthesis, stability in the membrane and stability in detergent micelles, we developed an …

A generic selection system for improved expression and thermostability of G protein-coupled receptors by directed evolution

C Klenk, J Ehrenmann, M Schütz, A Plückthun - Scientific reports, 2016 - nature.com
Structural and biophysical studies as well as drug screening approaches on G protein-
coupled receptors (GPCRs) have been largely hampered by the poor biophysical properties …

Conformational ensemble view of G protein-coupled receptors and the effect of mutations and ligand binding

R Abrol, SK Kim, JK Bray, B Trzaskowski… - Methods in …, 2013 - Elsevier
G protein-coupled receptors (GPCRs) are integral membrane proteins that can convert an
extracellular signal into multiple intracellular signaling processes. This pleiotropy of GPCRs …

The second extracellular loop: a damper for G protein–coupled receptors?

D Massotte, BL Kieffer - Nature structural & molecular biology, 2005 - nature.com
The second extracellular loop: a damper for G protein–coupled receptors? | Nature Structural
& Molecular Biology Skip to main content Thank you for visiting nature.com. You are using a …

Constitutively active G protein-coupled receptor mutants: implications on receptor function and drug action

S Cotecchia, F Fanelli, T Costa - Assay and drug development …, 2003 - liebertpub.com
Mutations of GPCRs can increase their constitutive (agonist-independent) activity. Some of
these mutations have been artificially introduced by site-directed mutagenesis; others occur …

Directed evolution of G-protein-coupled receptors for high functional expression and detergent stability

KM Schlinkmann, A Plückthun - Methods in enzymology, 2013 - Elsevier
G-protein-coupled receptors (GPCRs) are cell-surface receptors exhibiting a key role in
cellular signal transduction processes, thus making them pharmacologically highly relevant …

Structure and function of peptide-binding G protein-coupled receptors

F Wu, G Song, C de Graaf, RC Stevens - Journal of Molecular Biology, 2017 - Elsevier
G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors and are
important human drug targets. Of the 826 human GPCRs, 118 of them recognize …

Interacting residues in an activated state of a G protein-coupled receptor

YH Lee, F Naider, JM Becker - Journal of Biological Chemistry, 2006 - ASBMB
Ste2p, the G protein-coupled receptor (GPCR) for the tridecapeptide pheromone α-factor of
Saccharomyces cerevisiae, was used as a model GPCR to investigate the role of specific …