1,4‐Dihydropyridines modulate GTP hydrolysis by Go in neuronal membranes

FEBS Letters

Dolphin, A.C.¹  Sweeney, M.I.¹ 

[1] Department of Pharmacology, Royal Free Hospital School of Medicine, Rowland Hill St., London NW3 2PF, UK

关键词: 1;    4-Dihydropyridine;    Calcium channel;    G-protein;    GTPase;    Go;    Baclofen;    GTP;    guanosine triphosphate;    GTPγS;    guanosine 5′-O-3-thiotriphosphate;    p[NH]ppA;    adenosine 5′-[β;    γ-imido] triphosphate;    202–791;    2;    6-dimethyl-3-nitro-5-isopropylcarboxylate-4-(2;    1;    3-benzoxadiazo-4-yl)-1;    4-dihydropyridine;    Bay K 8644;    2;    6-dimethyl-3-nitro-5-methylcarboxylate4-(2-tri-fluoromethylphenyl)-1;    4-dihydropyridine;    PN 200-110;    2;    6-dimethyl-3-isopropyl-carboxylate-5-carbomethoxy-4-(2;    1;    3-benzoxadiazo-4-yl)-1;    4-dihydropyridine;    4-chloro-nifedipine;    2;    6-dimethyl-3;    5-dicarbomethoxy-4-(4-chlorophenyl)-1;    4-dihydropyridine;   

DOI  :  10.1016/0014-5793(92)81148-F

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Several lines of evidence suggest that L-type Cu²⁺ channels (1,4-dihydropyridine receptors) are modulated by GTP-binding, proteins. We have further examined this interaction by measuring the effect of 1,4-dihydropyridines on GTPase activity in brain membranes. Dihydropyridine agonists significantly increased OTPase, reflected by an increase in the maximal rate of GTP hydrolysis, without affecting the affinity for GTP or the binding of a non-hydrolysable analogue of GTP. The stimulating effect on GTPase was abolished by antisera raised against G_oα but not G_iα. L-type Ca²⁺ channels may act as endogenous GTPase activating proteins (GAPS) to stimulate GTP hydrolysis by G_o.

【 授权许可】

Unknown