※C&EN: LOOK BACK AT 2007.
C&EN steps back in time to look at research advances from a decade ago.
December 18, 2017 Volume 95 Issue 49

"G PROTEIN-COUPLED RECEPTOR STRUCTURES AIDED DRUG DESIGN"
A decade after a key structural analysis, scientists have a better understanding of the pharmaceutically important family of receptor proteins.

G protein-coupled receptors, or GPCRs, are the largest family of human proteins, with over 800 members.
They reside within cell membranes, receiving molecular signals from outside the cell and translating them into signals that influence cellular pathways inside the cell.
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Chris Tate of MRC Laboratory of Molecular Biology and coworkers had earlier used point mutations to stabilize GPCRs without disrupting the proteins’ conformations or functions.
The researchers, including Gebhard Schertler, obtained a GPCR structure with the method in 2008.
Heptares Therapeutics later obtained rights to that method.
Now called StaR, this approach has helped researchers obtain a number of GPCR structures.
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The benefits of GPCR structural information continue to grow.
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Crystal structures also helped Heptares design the GPCR-based drug candidate AZD4635, which AstraZeneca is testing to treat cancer.

“The past 10 years have seen dramatic improvements in our ability to solve X-ray structures of GPCRs and utilize these for drug design,”
says Fiona Marshall, director and chief scientific officer of Heptares.
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https://cen.acs.org/articles/95/i49/look-back-at-2007.html#Reversing-Rett-syndrome-in-mice-gave-hope-for-treatments