Herring B P, Fitzsimons D P, Stull J T, Gallagher P J
Department of Physiology, University of Texas Southwestern Medical Center, Dallas 75235-9040.
J Biol Chem. 1990 Sep 25;265(27):16588-91.
Myosin light chain kinase is a Ca2+/calmodulin-dependent protein kinase which exhibits a very high degree of protein substrate specificity. The regulatory light chain of myosin is the only known physiological substrate of the enzyme. Based upon epitope mapping of monoclonal antibodies which inhibit kinase activity competitively with respect to the light chain substrate, residues 235-319 of the rabbit skeletal muscle kinase have been proposed to contain a light chain-binding site (Herring, B. P., Stull, J. T., and Gallagher, P. J. (1990) J. Biol. Chem. 265, 1724-1730). With the expression of a truncated kinase, we have further localized this putative binding site to residues 235-294. Mutation of acidic residues at positions 269 and 270 of the kinase resulted in a 10-fold increase in the Km value for the myosin light chain, with no significant change in the Vmax value. In contrast, altering a cluster of acidic amino acids at positions 261-263 had little effect on the Km value for the myosin light chain. These results suggest that residues 269 and 270 may be involved in protein-substrate binding. Interestingly, these residues, located amino-terminal of the homologous catalytic core (positions 302-539), are in a region which is highly conserved among myosin light chain kinases, but not other protein kinases. It is probable that the homologous catalytic core contains structural elements required for phosphotransferase activity. The catalytic domain of myosin light chain kinase would therefore include these conserved elements together with additional specific substrate-binding residues.
肌球蛋白轻链激酶是一种依赖Ca2+/钙调蛋白的蛋白激酶,对蛋白质底物具有高度特异性。肌球蛋白的调节轻链是该酶唯一已知的生理底物。基于对与轻链底物竞争性抑制激酶活性的单克隆抗体的表位作图,有人提出兔骨骼肌激酶的235 - 319位残基包含一个轻链结合位点(赫林,B.P.,斯图尔,J.T.,和加拉格尔,P.J.(1990)《生物化学杂志》265,1724 - 1730)。通过表达截短的激酶,我们进一步将这个假定的结合位点定位到235 - 294位残基。激酶269和270位的酸性残基突变导致肌球蛋白轻链的Km值增加10倍,而Vmax值无显著变化。相反,改变261 - 263位的一簇酸性氨基酸对肌球蛋白轻链的Km值影响很小。这些结果表明269和270位残基可能参与蛋白质 - 底物结合。有趣的是,这些位于同源催化核心(302 - 539位)氨基末端的残基,处于肌球蛋白轻链激酶中高度保守但其他蛋白激酶中不保守的区域。同源催化核心可能包含磷酸转移酶活性所需的结构元件。因此,肌球蛋白轻链激酶的催化结构域将包括这些保守元件以及额外的特异性底物结合残基。