Vasella Andrea, Davies Gideon J, Böhm Matthias
Laboratorium für Organische Chemie, ETH Hönggerberg, HCI H317, CH-8093 Zürich, Switzerland.
Curr Opin Chem Biol. 2002 Oct;6(5):619-29. doi: 10.1016/s1367-5931(02)00380-0.
The three-dimensional structure of glycosidases and of their complexes and the study of transition-state mimics reveal structural details that correlate with mechanism. Of particular interest are the transition-state conformations harnessed by individual enzymes and the substrate distortion observed in enzyme-ligand complexes. 3D-structure in synergy with transition-state mimicry opens the way for mechanistic interpretation of enzyme inhibition and for the development of therapeutic agents.
糖苷酶及其复合物的三维结构以及过渡态类似物的研究揭示了与机制相关的结构细节。特别令人感兴趣的是各个酶所利用的过渡态构象以及在酶 - 配体复合物中观察到的底物畸变。三维结构与过渡态模拟协同作用,为酶抑制的机制解释和治疗药物的开发开辟了道路。