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Scientists unveil structure of molecular target of many drugs
Date:10/29/2007

he major challenges in the new study was getting enough of the beta2-adrenergic receptor protein to work with.

After trying in vain to get the protein in its natural form to crystallize, Brian Kobilka and co-workers at Stanford University turned to protein engineering. To overcome problems with the proteins floppiness, they replaced a flexible loop with a more rigid protein structure. Raymond Stevens and co-workers of The Scripps Research Institute managed to coax the intransigent proteins into tiny crystals by devising techniques and environmental conditions that mimicked the proteins native, membrane-like environment. These genetic engineering and crystallization techniques may be broadly applicable to similar proteins, paving the way for more structures from the hundreds of GPCRs encoded in the human genome.

This is an absolutely remarkable advance, said Jeremy M. Berg, Ph.D., director of NIGMS, which, in addition to spearheading the PSI, plays a leading role in the membrane protein Roadmap initiative. Many laboratories around the world are trying to reveal the secrets of these proteins, and this important structure takes the field to a higher level.


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Contact: Emily Carlson
carlsone@nigms.nih.gov
301-496-7301
NIH/National Institute of General Medical Sciences  
Source:Eurekalert

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Scientists unveil structure of molecular target of many drugs
Scientists unveil structure of molecular target of many drugs