New York Structural Biology Center, New York, New York 10027, USA.
J Med Chem. 2012 Nov 26;55(22):10282-6. doi: 10.1021/jm300871x. Epub 2012 Nov 12.
Human acetylcholinesterase (AChE) is a significant target for therapeutic drugs. Here we present high resolution crystal structures of human AChE, alone and in complexes with drug ligands; donepezil, an Alzheimer's disease drug, binds differently to human AChE than it does to Torpedo AChE. These crystals of human AChE provide a more accurate platform for further drug development than previously available.
人类乙酰胆碱酯酶(AChE)是治疗药物的重要靶点。在此,我们呈现了人类 AChE 的高分辨率晶体结构,包括单独存在和与药物配体结合的结构;用于治疗阿尔茨海默病的药物多奈哌齐与人类 AChE 的结合方式与它与 Torpedo AChE 的结合方式不同。这些人类 AChE 的晶体为进一步的药物开发提供了比以前更准确的平台。