The staudinger ligation

C Bednarek, I Wehl, N Jung, U Schepers… - Chemical …, 2020 - ACS Publications
While the Staudinger reaction has first been described a hundred years ago in 1919, the
ligation reaction became one of the most important and efficient bioconjugation techniques …

GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …

Bioorthogonal reactions of triarylphosphines and related analogues

TK Heiss, RS Dorn, JA Prescher - Chemical reviews, 2021 - ACS Publications
Bioorthogonal phosphines were introduced in the context of the Staudinger ligation over 20
years ago. Since that time, phosphine probes have been used in myriad applications to tag …

Conformational rearrangement during activation of a metabotropic glutamate receptor

BW Liauw, HS Afsari, R Vafabakhsh - Biophysical Journal, 2021 - cell.com
The ability to sense external stimuli and dynamically respond lies at the core of cellular
homeostasis. G protein-coupled receptors (GPCRs), the largest family of membrane proteins …

Labeling and single-molecule methods to monitor G protein-coupled receptor dynamics

H Tian, A Furstenberg, T Huber - Chemical reviews, 2017 - ACS Publications
The superfamily of G protein-coupled receptors (GPCRs) mediates a wide range of
physiological responses and serves as an important category of drug targets. Earlier …

Ghrelin receptor conformational dynamics regulate the transition from a preassembled to an active receptor: Gq complex

M Damian, S Mary, M Maingot… - Proceedings of the …, 2015 - National Acad Sciences
How G protein-coupled receptor conformational dynamics control G protein coupling to
trigger signaling is a key but still open question. We addressed this question with a model …

A molecular engineering toolbox for the structural biologist

GT Debelouchina, TW Muir - Quarterly reviews of biophysics, 2017 - cambridge.org
Exciting new technological developments have pushed the boundaries of structural biology,
and have enabled studies of biological macromolecules and assemblies that would have …

Mechanism of sensitivity modulation in the calcium-sensing receptor via electrostatic tuning

MR Schamber, R Vafabakhsh - Nature communications, 2022 - nature.com
Transfer of information across membranes is fundamental to the function of all organisms
and is primarily initiated by transmembrane receptors. For many receptors, how ligand …

Genetically encoding a light switch in an ionotropic glutamate receptor reveals subunit-specific interfaces

S Zhu, M Riou, CA Yao, S Carvalho… - Proceedings of the …, 2014 - National Acad Sciences
Reprogramming receptors to artificially respond to light has strong potential for molecular
studies and interrogation of biological functions. Here, we design a light-controlled …

Conformational fingerprinting of allosteric modulators in metabotropic glutamate receptor 2

BWH Liauw, A Foroutan, MR Schamber, W Lu… - Elife, 2022 - elifesciences.org
Activation of G protein-coupled receptors (GPCRs) is an allosteric process. It involves
conformational coupling between the orthosteric ligand binding site and the G protein …