The effects of charge-neutralizing mutation D6.30N on the functions of CB1 and CB2 cannabinoid receptors.
The effects of charge-neutralizing mutation D6.30N on the functions of CB1 and CB2 cannabinoid receptors.
复制标题
电荷中和突变 D6.30N 对 CB1 和 CB2 大麻素受体功能的影响。
DOI：
10.1016/j.febslet.2006.09.001
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发表时间：
2006
期刊：
影响因子：
3.5
通讯作者：
Song,Zhao-Hui
中科院分区：
文献类型：
--
作者：
Nebane,NtsangM;Kellie,Brandon;Song,Zhao-Hui
Charge-neutralizing mutation D6.30N of the human cannabinoid receptor subtype 1 (CB1) and cannabinoid receptor subtype 2 (CB2) cannabinoid receptors was made to test two hypotheses: (1) D6.30 may be crucial for the functions of CB1 and CB2 receptors. (2) D6.30 may participate in an ionic lock with R3.50 that keeps the receptors in an inactive conformation. Specific ligand binding and ligand-induced inhibition of forskolin-stimulated cAMP accumulation were observed with human embryonic kidney epithelial cell line (HEK293) cells expressing wild-type CB1 and CB2, as well as CB1D6.30N and CB2D6.30N mutant receptors. There was however a decrease in maximum response of the mutant receptors compared to their wild-type counterparts, suggesting that D6.30 is essential for full activation of both CB1 and CB2 receptors. Both CB1D6.30N and CB2D6.30N demonstrated a level of constitutive activity no greater than that of their wild-type counterparts, indicating that either D6.30 does not participate in a salt bridge with R3.50, or the salt bridge is not critical for keeping cannabinoid receptors in the inactive conformation.
