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铍中毒。酪蛋白激酶1的选择性抑制。

Beryllium toxicity. The selective inhibition of casein kinase 1.

作者信息

Cummings B, Kaser M R, Wiggins G, Ord M G, Stocken L A

出版信息

Biochem J. 1982 Oct 15;208(1):141-6. doi: 10.1042/bj2080141.

Abstract
  1. Cyclic AMP-independent casein kinase 1 in liver cytoplasm and nuclei was inhibited by Be2+ in vitro (Ki 2.5 microM and 29 microM respectively). Casein kinase 2 (phosvitin kinase) and cyclic AMP-dependent protein kinase were unaffected. 2. The inhibition of casein kinase 1 by Be2+ was competitive with respect to the protein substrate; at non-saturating concentrations of casein, inhibition was non-competitive with respect to ATP. 3. In rats given LD50 doses of Be2+ 24 h before death, the activities of cytoplasmic and nuclear casein kinase 1 in livers from partially hepatectomized animals were diminished approx. 50%; with intact rats, nuclear casein kinase 1 was inhibited at concentrations of casein less than the Km.
摘要
  1. 体外实验中,Be2+可抑制肝细胞质和细胞核中不依赖环磷酸腺苷(cAMP)的酪蛋白激酶1(Ki分别为2.5微摩尔/升和29微摩尔/升)。酪蛋白激酶2(磷蛋白激酶)和依赖环磷酸腺苷的蛋白激酶未受影响。2. Be2+对酪蛋白激酶1的抑制作用在蛋白质底物方面具有竞争性;在酪蛋白非饱和浓度下,对三磷酸腺苷(ATP)而言抑制作用无竞争性。3. 在死亡前24小时给予半数致死剂量Be2+的大鼠中,部分肝切除动物肝脏中细胞质和细胞核酪蛋白激酶1的活性降低约50%;对于完整大鼠,当酪蛋白浓度低于米氏常数(Km)时,细胞核酪蛋白激酶1受到抑制。

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本文引用的文献

6
The toxicity of beryllium.
Lab Invest. 1966 Jan;15(1 Pt 1):176-80.
10
A simple procedure for the purification of rat liver phosvitin kinase.
Biochim Biophys Acta. 1970 Sep 16;212(3):515-7. doi: 10.1016/0005-2744(70)90261-5.

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