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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

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

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

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.

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。

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

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

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.

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。