Roles of ring C oxygens in the binding of colchicine to tubulin.
Roles of ring C oxygens in the binding of colchicine to tubulin.
复制标题
C 环氧在秋水仙碱与微管蛋白结合中的作用。
DOI：
10.1021/bi00229a026
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发表时间：
1991
期刊：
影响因子：
2.9
通讯作者：
Timasheff,SN
中科院分区：
文献类型：
--
作者：
Medrano,FJ;Andreu,JM;Gorbunoff,MJ;Timasheff,SN
F. Javier Medrano，8 José M.安德鲁，8玛丽娜J Gorbunoff，”和Serge N。Timasheff*”Centro de Investigaciones Biológicas，Consejo上级de Investigaciones Científicas，28006马德里，西班牙，and Graduate Department of Biochemistry，Brandeis University，Waltham，马萨诸塞州02254接收于1990年8月9日;修订版Mandarpt接收于1990年11月29日摘要：通过研究2，3，4，4 ′-四甲氧基-1，3，4，4 ′-四甲氧基-1，4 ′-四甲氧基-1，4 ′-四甲氧基-1，4 ′-二羟基秋水仙碱联苯类似物与微管蛋白的相互作用，探讨了秋水仙碱C环氧在其与微管蛋白结合中的作用。1 ′-联苯（TMB）和2，3，4-三甲氧基-4 ′-乙酰基-1，1 ′-联苯（TKB），第一种在4 ′位含有甲氧基，第二种含有酮基。这两种类似物被发现在一个快速可逆的平衡特异性结合到微管蛋白上的秋水仙碱结合位点。25 ℃时的标准结合自由能为（7（？）
F. Javier Medrano, 8 José M. Andreu, 8 Marina J. Gorbunoff," and Serge N. Timasheff*·" Centro de Investigaciones Biológicas, Consejo Superior de Investigaciones Científicas, 28006 Madrid, Spain, and Graduate Department of Biochemistry, Brandéis University, Waltham, Massachusetts 02254 Received August 9, 1990; Revised Manuscript Received November 29, 1990 abstract: The roles of the oxygens in ring C of colchicine in its binding to tubulin were probed by a study of the interactions of two allocolchicine biphenyl analogues, 2, 3, 4, 4'-tetramethoxy-1, 1'-biphenyl (TMB) and 2, 3, 4-trimethoxy-4'-acetyl-1, 1'-biphenyl (TKB), the first one containing a methoxy group in position 4', the second a keto group. Both analogues were found to bind specifically to the colchicine-binding site on tubulin in a rapidly reversible equilibrium. The standard free energies of binding at 25 C were (7 ()