Beta-2 Adrenergic Receptor

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Solved Structure of a Beta 2-Adrenergic Receptor, (2rh1)


Contents

3D structures of beta-2 adrenergic receptor

 

β2 adrenergic receptor binding a hormone analog
and complexed to a heterotrimeric G protein (3sn6)

 

An activated G protein-coupled receptor (human β-2 adrenergic receptor in blue ) in a complex with a heterotrimeric G protein (3 subunits:reddish to orange-brown) and hormone (gold) (3sn6), resolution 3.2Å. The boundaries of the membrane in which the GPCR sits are represented in light green.


Adrenergic receptor

Nobel Prize Related to the Structures

Robert J. Lefkowitz and Brian K. Kobilka share the 2012 Nobel Prize in Chemistry for work on GPCRs that includes solving the first structures of a ligand-activated GPCR (2r4r, 2r4s, & 2rh1 in 2007)[1][2][3] and the first activated GPCR in complex with its G protein (3sn6 in 2011)[4][5][6][7]. A detailed description of the laureates' body of work on this class of receptors with images is here.

References

  1. 1.0 1.1 1.2 Witter FR, Zimmerman AW, Reichmann JP, Connors SL. In utero beta 2 adrenergic agonist exposure and adverse neurophysiologic and behavioral outcomes. Am J Obstet Gynecol. 2009 Dec;201(6):553-9. PMID:19961985 doi:10.1016/j.ajog.2009.07.010
  2. 2.0 2.1 Mehler MF, Purpura DP. Autism, fever, epigenetics and the locus coeruleus. Brain Res Rev. 2009 Mar;59(2):388-92. Epub 2008 Nov 24. PMID:19059284 doi:10.1016/j.brainresrev.2008.11.001
  3. Rasmussen SG, Choi HJ, Rosenbaum DM, Kobilka TS, Thian FS, Edwards PC, Burghammer M, Ratnala VR, Sanishvili R, Fischetti RF, Schertler GF, Weis WI, Kobilka BK. Crystal structure of the human beta2 adrenergic G-protein-coupled receptor. Nature. 2007 Nov 15;450(7168):383-7. Epub 2007 Oct 21. PMID:17952055 doi:10.1038/nature06325
  4. Cherezov V, Rosenbaum DM, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, Choi HJ, Kuhn P, Weis WI, Kobilka BK, Stevens RC. High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science. 2007 Nov 23;318(5854):1258-65. Epub 2007 Oct 25. PMID:17962520
  5. Hanson MA, Cherezov V, Griffith MT, Roth CB, Jaakola VP, Chien EY, Velasquez J, Kuhn P, Stevens RC. A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor. Structure. 2008 Jun;16(6):897-905. PMID:18547522 doi:10.1016/j.str.2008.05.001
  6. Scheerer P, Park JH, Hildebrand PW, Kim YJ, Krauss N, Choe HW, Hofmann KP, Ernst OP. Crystal structure of opsin in its G-protein-interacting conformation. Nature. 2008 Sep 25;455(7212):497-502. PMID:18818650 doi:10.1038/nature07330
  7. Warne T, Moukhametzianov R, Baker JG, Nehme R, Edwards PC, Leslie AG, Schertler GF, Tate CG. The structural basis for agonist and partial agonist action on a beta(1)-adrenergic receptor. Nature. 2011 Jan 13;469(7329):241-4. PMID:21228877 doi:10.1038/nature09746
  8. Cruickshank JM. Beta blockers in hypertension. Lancet. 2010 Aug 7;376(9739):415; author reply 415-6. PMID:20692524 doi:10.1016/S0140-6736(10)61217-2

See Also

External Resources

Page Development

This article was initially developed based on lectures given in Chemistry 543 by Prof. Clarence E. Schutt at Princeton University.

Proteopedia Page Contributors and Editors (what is this?)

Wayne Decatur, David Canner, Dotan Shaniv, Michal Harel

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