Guanine nucleotide‐ and GTP‐dependent N6‐phenylisopropyladenosine stimulation of the membrane‐bound cyclic AMP high affinity phosphodiesterase in rat brain

FEBS Letters

de Mazancourt, Philippe¹  Giudicelli, Yves¹ 

[1] Service de Biochimie de la Faculté de Médecine de Paris-Ouest et du Centre Hospitalier de Poissy, 78303 Poissy Cédex, France

关键词: Membrane-bound phosphodiesterase;    Guanine nucleotide;    Adenosine analog;    Guanine nucleotide regulatory protein;    Brain cortex;   

DOI  :  10.1016/0014-5793(84)80849-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

In brain cortex, low concentrations of GTP or Gpp(NH)p activated the membrane-bound low K _m cyclic AMP phosphodiesterase while higher concentrations of GTP, but not of Gpp(NH)p, reversed this activation. The adenosine analog N ⁶-phenylisopropyladenosine (N ⁶-PIA) elicited biphasic effect on this enzyme (activation up to 10⁻⁸ M, complete reversion at 10⁻⁵ M), provided that GTP was present. N ⁶-PIA activation was reduced in the presence of Gpp(NH)p and blocked by sodium (80 mM). In contrast, the soluble low K _m cyclic AMP phosphodiesterase was insensitive to GTP or N ⁶-PIA. This study suggests that guanine nucleotides and N ⁶-PIA exert their effects on the membrane-bound enzyme through guanine nucleotide regulatory proteins.

【 授权许可】

Unknown