Subunit dissociation as a possible mechanism of glucocorticoid receptor activation.

Subunit dissociation as a possible mechanism of glucocorticoid receptor activation.
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亚基解离是糖皮质激素受体激活的可能机制。

DOI:
10.1021/bi00277a038
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发表时间:
1983
期刊:
影响因子:
2.9
通讯作者:
W. Vedeckis
W. Vedeckis
中科院分区:
生物学3区
文献类型:
--
作者:
W. Vedeckis

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为了阐明类固醇激素受体活化的机制,测定了小鼠AtT-20垂体瘤细胞系中非蛋白水解糖皮质激素受体的未活化和活化形式的流体动力学性质。未活化的、稳定的受体具有以下性质:沉降系数= 9 S; Rs = 8.3 nm; Mr = 317 000; f/f0 = 1.70;轴比(长椭圆体)= 14。活化的单体受体的沉降系数为3.2 S,斯托克斯半径为6 nm,分子量为81 000,摩擦比为1.93,轴比(长椭圆体)为18。当在含有0.3 M KCl和20 mM Na 2 MoO 4的缓冲液中进行分析时,检测到中等大小的受体种类。其特征如下:沉降系数= 5 S; Rs = 8.3 nm; Mr = 176 000; f/f0 = 2.06;轴比(长椭圆体)= 22。初步研究似乎表明,这是一种激活形式的受体。根据分子量,很可能未活化的受体是相同的受体结合亚基(Mr = 81 000)的四聚体,而中间形式是同源二聚体。或者,非激素结合成分(受体结合因子)可能参与形成多聚体、非活化受体复合物。在任何一种情况下,多聚体的非活化受体解离成亚基似乎是受体活化的一种可能机制。最后,添加高浓度的1-硫代甘油促进活化。因此,巯基可能参与受体亚基相互作用。
For the elucidation of the mechanism of steroid hormone receptor activation, the hydrodynamic properties of the unactivated and activated forms of the nonproteolyzed glucocorticoid receptor from the mouse AtT-20 pituitary tumor cell line were determined. The unactivated, molybdate-stabilized receptor has the following properties: sedimentation coefficient = 9 S; Rs = 8.3 nm; Mr = 317 000; f/f0 = 1.70; axial ratio (prolate ellipsoid) = 14. The activated monomeric receptor has a sedimentation coefficient of 3.2 S, a Stokes radius of 6 nm, a molecular weight of 81 000, a frictional ratio of 1.93, and an axial ratio (prolate ellipsoid) of 18. A receptor species of intermediate size was detected when the analysis was performed in buffer containing both 0.3 M KCl and 20mM Na2MoO4. Its characteristics are as follows: sedimentation coefficient = 5 S; Rs = 8.3 nm; Mr = 176 000; f/f0 = 2.06; axial ratio (prolate ellipsoid) = 22. A preliminary study seemed to indicate that this is an activated form of the receptor. On the basis of the molecular weights, it is likely that the unactivated receptor is a tetramer of identical hormone-binding subunits (Mr = 81 000) while the intermediate form is a homodimer. Alternatively, non-hormone-binding components (receptor-binding factors) may be involved in forming the multimeric, nonactivated receptor complex. In either case, the dissociation of a multimeric, nonactivated receptor into subunits appears to be a possible mechanism of receptor activation. Finally, the addition of high concentrations of 1-thioglycerol promoted activation. Thus, sulfhydryl groups may be involved in receptor subunit interaction.
钼酸盐对糖皮质激素受体不同分子形式的可逆作用的物理化学分析。
DOI: 10.1016/0006-291x(81)91660-0
发表时间: 1981
影响因子: 3.1
作者:
Hutchens,TW;Markland,FS;Hawkins,EF
通讯作者: Hawkins,EF
小牛肠道碱性磷酸酶、磷酸酶抑制剂和磷酸化化合物对糖皮质激素受体复合物激活率的影响。
DOI: 10.1021/bi00564a046
发表时间: 1980
期刊: Biochemistry
影响因子: 2.9
作者:
Barnett,CA;Schmidt,TJ;Litwack,G
通讯作者: Litwack,G
鉴定可将雄激素受体的 4.5S 形式转化为 8S 的 8S 雄激素受体促进因子。
DOI: 10.1210/endo-109-2-496
发表时间: 1981
期刊: Endocrinology
影响因子: 4.8
作者:
Colvard,DS;Wilson,EM
通讯作者: Wilson,EM
DOI: 10.1016/0022-4731(80)90260-5
发表时间: 1980
期刊: Journal of steroid biochemistry
影响因子: --
作者:
Grody,WW;Compton,JG;Schrader,WT;O'Malley,BW
通讯作者: O'Malley,BW
肝脏和肾脏糖皮质激素受体复合物的激活发生在体内。
DOI: 10.1016/0003-9861(80)90440-3
发表时间: 1980
影响因子: 3.9
作者:
Marković,RD;Litwack,G
通讯作者: Litwack,G