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Structural basis for the activation and ligand recognition of the human oxytocin receptor

Here, Waltenspühl et al. report the cryo-EM structure of active human oxytocin receptor in complex with oxytocin and with a heterotrimeric G protein, providing insights into this hormone system critically involved in the regulation of social behaviour and reproduction.

Yann Waltenspühl
Janosch Ehrenmann
Andreas Plückthun
ResearchOpen Access18 Jul 2022
Nature Communications

Volume: 13, P: 1-9
Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists

Neurokinin receptors are G protein-coupled receptors. Here the authors present three crystal structures of the neurokinin 1 receptor (NK₁R) in complex with small-molecule antagonists including aprepitant and netupitant and observe that these clinically approved compounds induce a conformational change in the receptor.

Jendrik Schöppe
Janosch Ehrenmann
Andreas Plückthun
ResearchOpen Access03 Jan 2019
Nature Communications

Volume: 10, P: 1-11
High-resolution crystal structure of parathyroid hormone 1 receptor in complex with a peptide agonist

This structure of human PTH1R, a key target for the treatment of osteoporosis, reveals the agonist binding mode and molecular details within conserved structural motifs critical for class B GPCR function.

Janosch Ehrenmann
Jendrik Schöppe
Andreas Plückthun
Research19 Nov 2018
Nature Structural & Molecular Biology

Volume: 25, P: 1086-1092
Universal platform for the generation of thermostabilized GPCRs that crystallize in LCP

Structural studies of GPCRs are limited by difficulties in obtaining well-diffracting crystals. This protocol describes how to generate and screen for mutants with better thermal stability that is indicative for successful crystallization in lipidic cubic phase.

Jendrik Schöppe
Janosch Ehrenmann
Andreas Plückthun
Protocols09 Feb 2022
Nature Protocols

Volume: 17, P: 698-726
A generic selection system for improved expression and thermostability of G protein-coupled receptors by directed evolution

Christoph Klenk
Janosch Ehrenmann
Andreas Plückthun
ResearchOpen Access18 Feb 2016
Scientific Reports

Volume: 6, P: 1-9
Directed evolution of G protein-coupled receptors in yeast for higher functional production in eukaryotic expression hosts

Marco Schütz
Jendrik Schöppe
Andreas Plückthun
ResearchOpen Access25 Feb 2016
Scientific Reports

Volume: 6, P: 1-16

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Structural basis for the activation and ligand recognition of the human oxytocin receptor

Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists

High-resolution crystal structure of parathyroid hormone 1 receptor in complex with a peptide agonist

Universal platform for the generation of thermostabilized GPCRs that crystallize in LCP

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

Directed evolution of G protein-coupled receptors in yeast for higher functional production in eukaryotic expression hosts

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