scholarly journals Seeing the insulin receptor in action

2018 ◽  
Vol 217 (5) ◽  
pp. 1555-1555
Author(s):  
Ben Short

Researchers use single-particle electron microscopy to visualize an insulin-induced conformational shift that leads to receptor activation.

2017 ◽  
Author(s):  
Sandra Markovic-Mueller ◽  
Edward Stuttfeld ◽  
Mayanka Asthana ◽  
Tobias Weinert ◽  
Spencer Bliven ◽  
...  

SUMMARYVascular Endothelial Growth Factors (VEGFs) regulate blood and lymph vessel development upon activation of three receptor tyrosine kinases (RTKs), VEGFR-1, −2, and −3. Partial structures of VEGFR/VEGF complexes based on single particle electron microscopy, small angle X-ray scattering, and X-ray crystallography revealed the location of VEGF binding and domain arrangement of individual receptor subdomains. Here we describe the structure of the full-length VEGFR-1 extracellular domain (ECD) in complex with VEGF-A at 4 Å resolution. We combined X-ray crystallography, single particle electron microscopy, and molecular modeling for structure determination and validation. The structure reveals the molecular details of ligand-induced receptor dimerization, in particular of homotypic receptor interactions in Ig-domains 4, 5, and 7. Functional analyses of ligand binding and receptor activation confirm the relevance of these homotypic contacts and identify them as potential therapeutic sites to allosterically inhibit VEGFR-1 activity.


ACS Nano ◽  
2021 ◽  
Author(s):  
Nesrine Aissaoui ◽  
Josephine Lai-Kee-Him ◽  
Allan Mills ◽  
Nathalie Declerck ◽  
Zakia Morichaud ◽  
...  

2010 ◽  
Vol 26 (3) ◽  
pp. 035002 ◽  
Author(s):  
Wooram Park ◽  
Dean R Madden ◽  
Daniel N Rockmore ◽  
Gregory S Chirikjian

2009 ◽  
Vol 102 (2-3) ◽  
pp. 189-196 ◽  
Author(s):  
Egbert J. Boekema ◽  
Mihaela Folea ◽  
Roman Kouřil

Biochemistry ◽  
2009 ◽  
Vol 48 (28) ◽  
pp. 6618-6623 ◽  
Author(s):  
Katarzyna B. Mościcka ◽  
Tomasz Krupnik ◽  
Egbert J. Boekema ◽  
Juke S. Lolkema

2008 ◽  
Vol 162 (2) ◽  
pp. 260-270 ◽  
Author(s):  
Lindsay A. Baker ◽  
John L. Rubinstein

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