2ki9

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Human cannabinoid receptor-2 helix 6

Structural highlights

2ki9 is a 1 chain structure with sequence from Homo sapiens. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:Solution NMR
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

CNR2_HUMAN Heterotrimeric G protein-coupled receptor for endocannabinoid 2-arachidonoylglycerol mediating inhibition of adenylate cyclase. May function in inflammatory response, nociceptive transmission and bone homeostasis.[1] [2] [3] [4]

Publication Abstract from PubMed

We detail the structure and dynamics of a synthetic peptide corresponding to transmembrane helix 6 (TMH6) of human cannabinoid receptor-2 (hCB2) in biomembrane-mimetic environments. The peptide's NMR structural biology is characterized by two alpha-helical domains bridged by a flexible, nonhelical hinge region containing a highly-conserved CWFP motif with an environmentally sensitive, Pro-based conformational switch. Buried within the peptide's flexible region, W(258) may hydrogen-bond with L(255) to help stabilize the Pro-kinked hCB2 TMH6 structure and position C(257) advantageously for interaction with agonist ligands. These characteristics of hCB2 TMH6 are potential structural features of ligand-induced hCB2 activation in vivo.

Structural biology of human cannabinoid receptor-2 helix 6 in membrane-mimetic environments.,Tiburu EK, Tyukhtenko S, Deshmukh L, Vinogradova O, Janero DR, Makriyannis A Biochem Biophys Res Commun. 2009 Jun 26;384(2):243-8. Epub 2009 May 3. PMID:19397896[5]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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References

  1. ↑ Tao Q, McAllister SD, Andreassi J, Nowell KW, Cabral GA, Hurst DP, Bachtel K, Ekman MC, Reggio PH, Abood ME. Role of a conserved lysine residue in the peripheral cannabinoid receptor (CB2): evidence for subtype specificity. Mol Pharmacol. 1999 Mar;55(3):605-13. PMID:10051546
  2. ↑ Feng W, Song ZH. Effects of D3.49A, R3.50A, and A6.34E mutations on ligand binding and activation of the cannabinoid-2 (CB2) receptor. Biochem Pharmacol. 2003 Apr 1;65(7):1077-85. PMID:12663043
  3. ↑ Kishimoto S, Gokoh M, Oka S, Muramatsu M, Kajiwara T, Waku K, Sugiura T. 2-arachidonoylglycerol induces the migration of HL-60 cells differentiated into macrophage-like cells and human peripheral blood monocytes through the cannabinoid CB2 receptor-dependent mechanism. J Biol Chem. 2003 Jul 4;278(27):24469-75. Epub 2003 Apr 23. PMID:12711605 doi:http://dx.doi.org/10.1074/jbc.M301359200
  4. ↑ Anand U, Otto WR, Sanchez-Herrera D, Facer P, Yiangou Y, Korchev Y, Birch R, Benham C, Bountra C, Chessell IP, Anand P. Cannabinoid receptor CB2 localisation and agonist-mediated inhibition of capsaicin responses in human sensory neurons. Pain. 2008 Sep 15;138(3):667-80. doi: 10.1016/j.pain.2008.06.007. Epub 2008 Aug, 9. PMID:18692962 doi:http://dx.doi.org/10.1016/j.pain.2008.06.007
  5. ↑ Tiburu EK, Tyukhtenko S, Deshmukh L, Vinogradova O, Janero DR, Makriyannis A. Structural biology of human cannabinoid receptor-2 helix 6 in membrane-mimetic environments. Biochem Biophys Res Commun. 2009 Jun 26;384(2):243-8. Epub 2009 May 3. PMID:19397896 doi:10.1016/j.bbrc.2009.04.099

Contents


PDB ID 2ki9

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