GPCR Structures - Human Histamine H1 receptor



Another GPCR paper published - this time for the human Histamine H1 receptor - the target of a large number of anti-inflammatory drugs. The structure is complexed with Doxepin, a ligand showing very broad pharmacology. Link to the paper is here.

This makes a total of eight sequence distinct (or seven paralogous) rhodopsin-like GPCRs in the public domain. These are:

  • rhodopsin (bovine and squid)
  • beta-2 adrenergic receptor (human)
  • beta-1 adrenergic receptor (turkey)
  • dopamine D3 receptor (human)
  • histamine H1 receptor (human)
  • adenosine A2a receptor (human)
  • CCR-4 (human)
The table of GPCR structures has been updated.

The structure is available on-line as PDBe:3rze, as for many other GPCR structures, it is an engineered lysozyme chimera, and diffracts to 3.1Å.

%T Structure of the human histamine H1 receptor complex with doxepin
%J Nature
%D 2011
%A T. Shimamura
%A M. Shiroishi
%A S. Weyand,  
%A H. Tsujimoto  
%A G. Winter
%A V. Katritch  
%A R. Abagyan  
%A V. Cherezov
%A W. Liu  
%A G.W. Han  
%A T. Kobayashi 
%A R.C. Stevens
%A S. Iwata
%O doi:10.1038/nature10236