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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 384 243-8 (2009)
Cited: 12 times
EuropePMC logo PMID: 19397896

Abstract

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.

Articles - 2ki9 mentioned but not cited (1)

  1. Selective Targeting of Lung Cancer Cells with Methylparaben-Tethered-Quinidine Cocrystals in 3D Spheroid Models. Krishnamoorthi S, Kasinathan GN, Paramasivam G, Rath SN, Prakash J. ACS Omega 8 46628-46639 (2023)


Reviews citing this publication (2)

  1. Challenges and Perspectives in Chemical Synthesis of Highly Hydrophobic Peptides. Mueller LK, Baumruck AC, Zhdanova H, Tietze AA. Front Bioeng Biotechnol 8 162 (2020)
  2. Invited review: GPCR structural characterization: Using fragments as building blocks to determine a complete structure. Cohen LS, Fracchiolla KE, Becker J, Naider F. Biopolymers 102 223-243 (2014)

Articles citing this publication (9)

  1. Crystal structures of agonist-bound human cannabinoid receptor CB1. Hua T, Vemuri K, Nikas SP, Laprairie RB, Wu Y, Qu L, Pu M, Korde A, Jiang S, Ho JH, Han GW, Ding K, Li X, Liu H, Hanson MA, Zhao S, Bohn LM, Makriyannis A, Stevens RC, Liu ZJ. Nature 547 468-471 (2017)
  2. Mass spectrometry-based proteomics of human cannabinoid receptor 2: covalent cysteine 6.47(257)-ligand interaction affording megagonist receptor activation. Szymanski DW, Papanastasiou M, Melchior K, Zvonok N, Mercier RW, Janero DR, Thakur GA, Cha S, Wu B, Karger B, Makriyannis A. J Proteome Res 10 4789-4798 (2011)
  3. hCB2 ligand-interaction landscape: cysteine residues critical to biarylpyrazole antagonist binding motif and receptor modulation. Mercier RW, Pei Y, Pandarinathan L, Janero DR, Zhang J, Makriyannis A. Chem Biol 17 1132-1142 (2010)
  4. NMR solution structure of human cannabinoid receptor-1 helix 7/8 peptide: candidate electrostatic interactions and microdomain formation. Tyukhtenko S, Tiburu EK, Deshmukh L, Vinogradova O, Janero DR, Makriyannis A. Biochem Biophys Res Commun 390 441-446 (2009)
  5. Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies. Lange JH, van der Neut MA, Wals HC, Kuil GD, Borst AJ, Mulder A, den Hartog AP, Zilaout H, Goutier W, van Stuivenberg HH, van Vliet BJ. Bioorg Med Chem Lett 20 1084-1089 (2010)
  6. Expression and biophysical analysis of a triple-transmembrane domain-containing fragment from a yeast G protein-coupled receptor. Caroccia KE, Estephan R, Cohen LS, Arshava B, Hauser M, Zerbe O, Becker JM, Naider F. Biopolymers 96 757-771 (2011)
  7. Large multiple transmembrane domain fragments of a G protein-coupled receptor: biosynthesis, purification, and biophysical studies. Potetinova Z, Tantry S, Cohen LS, Caroccia KE, Arshava B, Becker JM, Naider F. Biopolymers 98 485-500 (2012)
  8. Dissimilar interaction of CB1/CB2 with lipid bilayers as revealed by molecular dynamics simulation. Ramos J, Cruz VL, Martínez-Salazar J, Campillo NE, Páez JA. Phys Chem Chem Phys 13 3660-3668 (2011)
  9. Expression, Purification, and Monitoring of Conformational Changes of hCB2 TMH67H8 in Different Membrane-Mimetic Lipid Mixtures Using Circular Dichroism and NMR Techniques. Tiburu EK, Zhuang J, Fleischer HN, Arthur PK, Awandare GA. Membranes (Basel) 7 E10 (2017)


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