Structure of the glucagon receptor in complex with a glucagon analogue

Journal: Nature

Published: 2018-01-04

DOI: 10.1038/nature25153

Affiliations: 19

Authors: 22

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Research Highlight

How receptors take shape

© MOLEKUUL/SCIENCE PHOTO LIBRARY/Getty

© MOLEKUUL/SCIENCE PHOTO LIBRARY/Getty

An international collaboration has determined the activated crystal structure of the human glucagon receptor — which plays a critical role in regulating blood sugar levels — in a complex with a partial activator.

The team, which includes ShanghaiTech University researchers, had previously reported glucagon receptor’s inactive structure. They have now compared the receptor’s inactive and active structures and discovered stark differences in shape, or conformation. This provides useful insights into the mechanics of molecule binding and activation. Two extracellular receptor segments, known as the stalk region and first extracellular loop, were found to play essential roles in recognizing glucagon, glucagon receptor’s natural physiological activator.

This discovery is set to benefit our understanding of G-protein coupled receptors, an important category of biological receptors to which glucagon receptor belongs.


Supported content

  1. Nature 553, 106−110 (2018). doi: 10.1038/nature25153
Institutions FC
CAS Key Laboratory of Receptor Research (CASKLRR), SIMM CAS, China 0.21
Novo Nordisk A/S, Denmark 0.14
University of Chinese Academy of Sciences (UCAS), China 0.10
National Center for Drug Screening, China 0.08
Department of Biochemistry, U of T, Canada 0.07
State Key Laboratory of Drug Research (SKLDR), SIMM CAS, China 0.06
CAS Center for Excellence in Biomacromolecules, China 0.05
GPCR Consortium, United States of America (USA) 0.05
Department of Pharmacology, ZZU, China 0.05
Shanghai Key Laboratory of Regulatory Biology, ECNU, China 0.05
School of Life Science and Technology (SLST), ShanghaiTech, China 0.04
National Laboratory of Biomacromolecules (NLB), IBP CAS, China 0.03
National Center for Protein Science Shanghai (NCPSS), SIBS CAS, China 0.03
Department of Molecular Genetics, U of T, Canada 0.02
iHuman Institute, ShanghaiTech, China 0.02
Drug Discovery and Design Center, SIMM CAS, China 0.01
School of Pharmacy, Fudan University, China 0.01

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