Koutalos Y, Nakatani K, Tamura T, Yau K W
Department of Neuroscience, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA.
J Gen Physiol. 1995 Nov;106(5):863-90. doi: 10.1085/jgp.106.5.863.
cGMP mediates vertebrate phototransduction by directly gating cationic channels on the plasma membrane of the photoreceptor outer segment. This second messenger is produced by a guanylate cyclase and hydrolyzed by a light-activated cGMP-phosphodiesterase. Both of these enzyme activities are Ca2+ sensitive, the guanylate cyclase activity being inhibited and the light-activated phosphodiesterase being enhanced by Ca2+. Changes in these activities due to a light-induced decrease in intracellular Ca2+ are involved in the adaptation of photoreceptors to background light. We describe here experiments to characterize the guanylate cyclase activity and its modulation by Ca2+ using a truncated rod outer segment preparation, in order to evaluate the enzyme's role in light adaptation. The outer segment of a tiger salamander rod was drawn into a suction pipette to allow recording of membrane current, and the remainder of the cell was sheared off with a probe to allow internal dialysis. The cGMP-gated channels on the surface membrane were used to monitor conversion of GTP, supplied from the bath, into cGMP by the guanylate cyclase in the outer segment. At nominal 0 Ca2+, the cyclase activity had a Km of 250 microM MgGTP and a Vmax of 25 microM cGMP s-1 in the presence of 1.6 mM free Mg2+; in the presence of 0.5 mM free Mg2+, the Km was 310 microM MgGTP and the Vmax was 17 microM cGMP s-1. The stimulation by Mg2+ had an EC50 of 0.2 mM Mg2+ for MgGTP at 0.5 mM. Ca2+ inhibited the cyclase activity. In a K+ intracellular solution, with 0.5 mM free Mg2+ and 2.0 mM GTP, the cyclase activity was 13 microM cGMP s-1 at nominal 0 Ca2+; Ca2+ decreased this activity with a IC50 of approximately 90 nM and a Hill coefficient of approximately 2.0.
环磷酸鸟苷(cGMP)通过直接开启光感受器外段质膜上的阳离子通道来介导脊椎动物的光转导。这种第二信使由鸟苷酸环化酶产生,并被光激活的cGMP磷酸二酯酶水解。这两种酶的活性都对Ca2+敏感,鸟苷酸环化酶活性被Ca2+抑制,而光激活的磷酸二酯酶活性被Ca2+增强。由于光诱导细胞内Ca2+减少而导致的这些活性变化参与了光感受器对背景光的适应。我们在此描述了使用截断的视杆外段制剂来表征鸟苷酸环化酶活性及其受Ca2+调节的实验,以评估该酶在光适应中的作用。将虎螈视杆的外段吸入吸管以记录膜电流,并用探针切断细胞的其余部分以进行内部透析。表面膜上的cGMP门控通道用于监测浴液中提供的GTP被外段中的鸟苷酸环化酶转化为cGMP的情况。在名义上0 Ca2+时,在存在1.6 mM游离Mg2+的情况下,环化酶活性的米氏常数(Km)为250 microM MgGTP,最大反应速度(Vmax)为25 microM cGMP s-1;在存在0.5 mM游离Mg2+的情况下,Km为310 microM MgGTP,Vmax为17 microM cGMP s-1。Mg2+的刺激对于0.5 mM的MgGTP,其半数有效浓度(EC50)为0.2 mM Mg2+。Ca2+抑制环化酶活性。在含有0.5 mM游离Mg2+和2.0 mM GTP的K+细胞内溶液中,在名义上0 Ca2+时,环化酶活性为13 microM cGMP s-1;Ca2+以约90 nM的半数抑制浓度(IC50)和约2.0的希尔系数降低该活性。