Semisynthetic derivatives of inositol 1,4,5-trisphosphate substituted at the 1-phosphate group. Effects on calcium release from permeabilized guinea-pig parotid acinar cells and comparison with binding to aldolase A.
Semisynthetic derivatives of inositol 1,4,5-trisphosphate substituted at the 1-phosphate group. Effects on calcium release from permeabilized guinea-pig parotid acinar cells and comparison with binding to aldolase A.
复制标题
肌醇 1,4,5-三磷酸酯的半合成衍生物，在 1-磷酸基团处被取代。
DOI：
--
复制
发表时间：
1988
期刊：
影响因子：
--
通讯作者：
H. Söling
中科院分区：
文献类型：
--
作者：
V. Henne;G. Mayr;B. Grabowski;B. Koppitz;H. Söling
本文比较了肌醇1，4，5-（三）磷酸[Ins（1，4，5）P_3]在磷酸1位上的取代衍生物对透化豚鼠腮腺腺泡细胞的钙释放作用和对醛缩酶A的抑制作用。sn-甘油（3）-1-磷酸-D-肌醇-4，5-（双）磷酸，以及乙醇醛（2）-1-磷酸-D-肌醇-4，5-（双）磷酸[GcaPIns（4，5）P2]及其衍生物N-辛基-氨基乙醇（1）-1-磷酸-D-肌醇-4，5-（双）磷酸刺激钙释放并抑制醛缩酶A。Ins（1，4，5）P3的不同衍生物的相对功效对于两种效应是相似的。N-羟乙基-2-氨基乙醇（1）-1-磷酸-D-肌醇-4，5-（双）磷酸[HeAetPIns（4，5）P2]（GcaPIns（4，5）P2的另一种衍生物）对两个参数的影响显著低于其他Ins（1，4，5）P3衍生物。虽然导致钙释放的半数最大激活的浓度从Ins（1，4，5）P3的1.7 μ M变化到HeAetPIns（4，5）P2的128 μ M，但所有衍生物的最大效应是相同的。结果表明，Ins（1，4，5）P3的1-磷酸基团可以被修饰，而没有或只有轻微的生物活性损失。这可用于未来的研究，旨在阐明推定的Ins（1，4，5）P3结合位点。
Derivatives of inositol 1,4,5-(tris)phosphate [Ins(1,4,5)P3] substituted at phosphate 1 were compared with respect to their calcium releasing effect in permeabilized guinea pig parotid acinar cells and to their inhibitory action on aldolase A. sn-Glycero(3)-1-phospho-D-myo-inositol-4,5-(bis)phosphate, but also glycolaldehyde(2)-1-phospho-D-myo-inositol-4,5-(bis)phosphate [GcaPIns(4,5)P2] and its derivative N-octyl-aminoethanol(1)-1-phospho-D-myo-inositol-4,5-(bis)phosphate stimulated calcium release and inhibited aldolase A. The relative efficacy of the different derivatives of Ins(1,4,5)P3 was similar for both effects. N-Hydroxyethyl-2-aminoethanol(1)-1-phospho-D-myo-inositol-4,5-(bis)phosp hate [HeAetPIns(4,5)P2], another derivative of GcaPIns(4,5)P2 was considerably less effective on both parameters than the other Ins(1,4,5)P3 derivatives. Although the concentration leading to half-maximal activation of calcium release varied from 1.7 microM for Ins(1,4,5)P3 to 128 microM for HeAetPIns(4,5)P2, the maximal effect was the same for all derivatives. The results indicate that the 1-phosphate group of Ins(1,4,5)P3 can be modified without or with only minor loss of biological activity. This may be utilized for future studies aiming at elucidating the putative Ins(1,4,5)P3 binding site.
肌醇 1,4,5-三磷酸。
DOI：
--
发表时间：
1984
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Joseph,SK;Thomas,AP;Williams,RJ;Irvine,RF;Williamson,JR
通讯作者：
Williamson,JR
洋地黄皂苷通透性胰岛模型。
DOI：
10.1042/bj2270965
发表时间：
1985
期刊：
The Biochemical journal
影响因子：
--
作者：
Wolf,BA;Comens,PG;Ackermann,KE;Sherman,WR;McDaniel,ML
通讯作者：
McDaniel,ML