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The cannabinoid type-1 receptor carboxyl-terminus, more than just a tail.
J Neurochem 2011; 117(1):1-18JN

Abstract

The cannabinoid type-1 (CB(1)) receptor is a G protein-coupled receptor that binds the main active ingredient of marijuana, Δ(9)-tetrahydrocannabinol, and has been implicated in several disease states, including drug addiction, anxiety, depression, obesity, and chronic pain. In the two decades since the discovery of CB(1), studies at the molecular level have centered on the transmembrane core. This interest has now expanded as we discover that other regions of CB(1), including the CB(1) carboxyl-terminus, have critical structures that are important for CB(1) activity and regulation. Following the recent description of the three dimensional structure of the full-length CB(1) carboxyl-terminal tail [Biopolymers (2009) vol. 91, pp. 565-573], several residues and structural motifs including two α-helices (termed H8 and H9) have been postulated to interact with common G protein-coupled receptor accessory proteins, such as G-proteins and β-arrestins. This discourse will focus on the CB(1) carboxyl-terminus; our current understanding of the structural features of this region, evidence for its interaction with proteins, and the impact of structure on the binding and regulatory function of CB(1) accessory proteins. The involvement of the carboxyl-terminus in the receptor life cycle including activation, desensitization, and internalization will be highlighted.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut, USA.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural
Review

Language

eng

PubMed ID

21244428

Citation

Stadel, Rebecca, et al. "The Cannabinoid Type-1 Receptor Carboxyl-terminus, More Than Just a Tail." Journal of Neurochemistry, vol. 117, no. 1, 2011, pp. 1-18.
Stadel R, Ahn KH, Kendall DA. The cannabinoid type-1 receptor carboxyl-terminus, more than just a tail. J Neurochem. 2011;117(1):1-18.
Stadel, R., Ahn, K. H., & Kendall, D. A. (2011). The cannabinoid type-1 receptor carboxyl-terminus, more than just a tail. Journal of Neurochemistry, 117(1), pp. 1-18. doi:10.1111/j.1471-4159.2011.07186.x.
Stadel R, Ahn KH, Kendall DA. The Cannabinoid Type-1 Receptor Carboxyl-terminus, More Than Just a Tail. J Neurochem. 2011;117(1):1-18. PubMed PMID: 21244428.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The cannabinoid type-1 receptor carboxyl-terminus, more than just a tail. AU - Stadel,Rebecca, AU - Ahn,Kwang H, AU - Kendall,Debra A, Y1 - 2011/02/11/ PY - 2011/1/20/entrez PY - 2011/1/20/pubmed PY - 2011/5/17/medline SP - 1 EP - 18 JF - Journal of neurochemistry JO - J. Neurochem. VL - 117 IS - 1 N2 - The cannabinoid type-1 (CB(1)) receptor is a G protein-coupled receptor that binds the main active ingredient of marijuana, Δ(9)-tetrahydrocannabinol, and has been implicated in several disease states, including drug addiction, anxiety, depression, obesity, and chronic pain. In the two decades since the discovery of CB(1), studies at the molecular level have centered on the transmembrane core. This interest has now expanded as we discover that other regions of CB(1), including the CB(1) carboxyl-terminus, have critical structures that are important for CB(1) activity and regulation. Following the recent description of the three dimensional structure of the full-length CB(1) carboxyl-terminal tail [Biopolymers (2009) vol. 91, pp. 565-573], several residues and structural motifs including two α-helices (termed H8 and H9) have been postulated to interact with common G protein-coupled receptor accessory proteins, such as G-proteins and β-arrestins. This discourse will focus on the CB(1) carboxyl-terminus; our current understanding of the structural features of this region, evidence for its interaction with proteins, and the impact of structure on the binding and regulatory function of CB(1) accessory proteins. The involvement of the carboxyl-terminus in the receptor life cycle including activation, desensitization, and internalization will be highlighted. SN - 1471-4159 UR - https://www.unboundmedicine.com/medline/citation/21244428/abstract/The_cannabinoid_type_1_receptor_carboxyl_terminus_more_than_just_a_tail_ L2 - https://doi.org/10.1111/j.1471-4159.2011.07186.x DB - PRIME DP - Unbound Medicine ER -