Copeland R A, Horiuchi K Y
Department of Chemical Enzymology, The DuPont Merck Research Laboratories, Wilmington, DE 19880-0400, USA.
Biochem Pharmacol. 1998 Jun 1;55(11):1785-90. doi: 10.1016/s0006-2952(97)00663-1.
Nonspecific protein binding is a commonly encountered problem with synthetic molecules designed as enzyme inhibitors. When the substrate for the enzymatic reaction is itself a protein, such nonspecific protein binding can also occur. Here, we demonstrate that this phenomenon can have a dramatic effect on the steady-state kinetic evaluation of such inhibitors.
非特异性蛋白质结合是设计为酶抑制剂的合成分子常见的问题。当酶促反应的底物本身是一种蛋白质时,也会发生这种非特异性蛋白质结合。在此,我们证明这种现象会对这类抑制剂的稳态动力学评估产生显著影响。