Taylor M G, Rajpal A, Kirsch J F
Center for Advanced Materials, Lawrence Berkeley National Laboratory, Berkeley, California 94720, USA.
Protein Sci. 1998 Sep;7(9):1857-67. doi: 10.1002/pro.5560070902.
The rate constants, k(on), for the formation of hen (chicken) lysozyme (HEWL). Fab-10 complexes have been determined for wild-type (WT) and epitope-mutated lysozymes by a homogeneous solution method based on the 95% reduced enzymatic activity of the complex. The values fall within a narrow 10-fold range [(0.18 to 1.92) x 10(6) M(-1)s(-l)]. The affinity constants, K(D), cover a broader, 440-fold, range from 0.075 to 33 nM. Values of K(D) as high as 7 microM were obtained for the complexes prepared from some mutations at HEWL positions 96 and 97, but the associated kinetic constants could not be determined. The values of k(on) are negatively correlated with side-chain volume at position 101HEWL, but are essentially independent of this parameter for position 21HEWL substitutions. The multiple mutations made at positions 21HEWL and 101HEWL provide sufficient experimental data on complex formation to evaluate phi values [phi = (deltadeltaGon)/(deltadeltaG(D))] at these two positions to begin to define trajectories for protein-protein association. The data, when interpreted within the concept of a two-step association sequence embracing a metastable encounter complex intermediate, argue that the rate determining step at position 21HEWL (phiavg = 0.2) is encounter complex formation, but the larger phi(avg) value of 0.36 experienced for most position 101HEWL mutations indicates a larger contribution from the post-encounter annealing process at this site for these replacements.
通过基于复合物95%酶活性降低的均相溶液法,测定了野生型(WT)和表位突变溶菌酶形成鸡(母鸡)溶菌酶(HEWL).Fab-10复合物的速率常数k(on)。这些值落在一个狭窄的10倍范围内[(0.18至1.92)×10(6) M(-1)s(-1)]。亲和常数K(D)涵盖了更宽的440倍范围,从0.075到33 nM。对于由HEWL第96和97位的一些突变制备的复合物,获得了高达7 μM的K(D)值,但相关的动力学常数无法确定。k(on)的值与HEWL第101位的侧链体积呈负相关,但对于HEWL第21位的取代,该参数基本无关。在HEWL第21位和第101位进行的多个突变提供了足够的复合物形成实验数据,以评估这两个位置的phi值[phi = (deltadeltaGon)/(deltadeltaG(D))],从而开始定义蛋白质-蛋白质结合的轨迹。当在包含亚稳态相遇复合物中间体的两步结合序列概念内解释这些数据时,表明HEWL第21位的速率决定步骤(phiavg = 0.2)是相遇复合物的形成,但对于大多数HEWL第101位突变所经历的较大phi(avg)值0.36表明,在该位点这些取代的相遇后退火过程贡献更大。