新霉素对锤头状核酶的抑制作用。
Inhibition of the hammerhead ribozyme by neomycin.
作者信息
Stage T K, Hertel K J, Uhlenbeck O C
机构信息
Department of Chemistry and Biochemistry, University of Colorado, Boulder 80309-0215, USA.
出版信息
RNA. 1995 Mar;1(1):95-101.
A series of antibiotics was tested for stimulation or inhibition of the hammerhead ribozyme cleavage reaction. Neomycin was found to be a potent inhibitor of the reaction with a Kl of 13.5 microM. Two hammerheads with well-characterized kinetics were used to determine which steps in the reaction mechanism were inhibited by neomycin. The data suggest that neomycin interacts preferentially with the enzyme-substrate complex and that this interaction leads to a reduction in the cleavage rate by stabilizing the ground state of the complex and destabilizing the transition state of the cleavage step. A comparison of neomycin with other aminoglycosides and inhibitors of hammerhead cleavage implies that the ammonium ions of neomycin are important for the antibiotic-hammerhead interaction.
测试了一系列抗生素对锤头状核酶切割反应的刺激或抑制作用。发现新霉素是该反应的有效抑制剂，其抑制常数（Kl）为13.5微摩尔。使用两个具有明确动力学特征的锤头状核酶来确定反应机制中的哪些步骤被新霉素抑制。数据表明，新霉素优先与酶-底物复合物相互作用，这种相互作用通过稳定复合物的基态和破坏切割步骤的过渡态来导致切割速率降低。新霉素与其他氨基糖苷类药物以及锤头状核酶切割抑制剂的比较表明，新霉素的铵离子对于抗生素与锤头状核酶的相互作用很重要。
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