Cooper David R, Boczek Tomasz, Grelewska Katarzyna, Pinkowska Malgorzata, Sikorska Malgorzata, Zawadzki Michal, Derewenda Zygmunt
Department of Molecular Physiology and Biological Physics and Integrated Center for Structure-Function Innovation, University of Virginia, Charlottesville, Virginia 22908-0736, USA.
Acta Crystallogr D Biol Crystallogr. 2007 May;63(Pt 5):636-45. doi: 10.1107/S0907444907010931. Epub 2007 Apr 21.
A strategy of rationally engineering protein surfaces with the aim of obtaining mutants that are distinctly more susceptible to crystallization than the wild-type protein has previously been suggested. The strategy relies on replacing small clusters of two to three surface residues characterized by high conformational entropy with alanines. This surface entropy reduction (or SER) method has proven to be an effective salvage pathway for proteins that are difficult to crystallize. Here, a systematic comparison of the efficacy of using Ala, His, Ser, Thr and Tyr to replace high-entropy residues is reported. A total of 40 mutants were generated and screened using two different procedures. The results reaffirm that alanine is a particularly good choice for a replacement residue and identify tyrosines and threonines as additional candidates that have considerable potential to mediate crystal contacts. The propensity of these mutants to form crystals in alternative screens in which the normal crystallization reservoir solutions were replaced with 1.5 M NaCl was also examined. The results were impressive: more than half of the mutants yielded a larger number of crystals with salt as the reservoir solution. This method greatly increased the variety of conditions that yielded crystals. Taken together, these results suggest a powerful crystallization strategy that combines surface engineering with efficient screening using standard and alternate reservoir solutions.
此前曾有人提出一种合理改造蛋白质表面的策略,目的是获得比野生型蛋白质明显更易于结晶的突变体。该策略依赖于用丙氨酸取代两到三个具有高构象熵特征的表面残基小簇。这种表面熵降低(或SER)方法已被证明是难以结晶的蛋白质的一种有效挽救途径。在此,报告了使用丙氨酸、组氨酸、丝氨酸、苏氨酸和酪氨酸取代高熵残基的效果的系统比较。总共生成了40个突变体,并使用两种不同程序进行筛选。结果再次证实丙氨酸是取代残基的特别好的选择,并确定酪氨酸和苏氨酸为具有相当大介导晶体接触潜力的额外候选者。还检查了这些突变体在将正常结晶储液替换为1.5 M NaCl的替代筛选中形成晶体的倾向。结果令人印象深刻:超过一半的突变体在以盐作为储液时产生了更多晶体。该方法大大增加了产生晶体的条件的多样性。综上所述,这些结果表明了一种强大的结晶策略,即将表面工程与使用标准和替代储液的高效筛选相结合。