Nichols R A, Shooter E M
J Biol Chem. 1983 Sep 10;258(17):10296-303.
The effect of the structural heterogeneity of the gamma subunit of 7 S nerve growth factor (NGF) on its interaction with a variety of synthetic substrates and natural ligands was studied. The major gamma species, distinguished on the basis of charge under isoelectric focusing conditions, were examined for possible differences in affinity toward basic pancreatic trypsin inhibitor, beta NGF, and 7 S NGF and differences in activity toward three synthetic arginine substrates, N alpha-benzoyl-DL-arginine-p-nitroanilide, p-tosyl-L-arginine methyl ester, N alpha-benzoyl-L-arginine ethyl ester. The most proteolytically modified form of the gamma subunit, gamma 3, was found to have an affinity for the natural ligands that was consistently an order of magnitude greater than gamma 1, the least modified form, while gamma 2 was intermediate, tending toward gamma 1. These differences were found to hold true for the activities toward the synthetic substrates as determined by the kcat/Km ratios. The nature of the affinity and activity differences among the major gamma species is discussed in light of a model where the presence or absence of certain basic residues, which along with the presence or absence of specific peptide chain cleavages forming the basis of the gamma subunit structural heterogeneity influence the access of ligand to the active site.
研究了7S神经生长因子(NGF)γ亚基的结构异质性对其与多种合成底物和天然配体相互作用的影响。在等电聚焦条件下根据电荷区分出主要的γ种类,检测它们对碱性胰蛋白酶抑制剂、β-NGF和7S-NGF的亲和力差异,以及对三种合成精氨酸底物(Nα-苯甲酰-DL-精氨酸对硝基苯胺、对甲苯磺酰-L-精氨酸甲酯、Nα-苯甲酰-L-精氨酸乙酯)的活性差异。发现γ亚基的最易被蛋白水解修饰的形式γ3对天然配体的亲和力始终比对修饰最少的形式γ1高一个数量级,而γ2处于中间水平,倾向于γ1。通过kcat/Km比值确定,这些差异在对合成底物的活性方面也成立。根据一个模型讨论了主要γ种类之间亲和力和活性差异的本质,在该模型中,某些碱性残基的存在与否,以及形成γ亚基结构异质性基础的特定肽链切割的存在与否,会影响配体与活性位点的结合。