Lundstrom Kenneth
BioXtal, Chemin des Croisettes 22, CH-1066 Epalinges, Switzerland.
Bioorg Med Chem Lett. 2005 Aug 15;15(16):3654-7. doi: 10.1016/j.bmcl.2005.05.041.
More than 60% of the current drugs are based on G protein-coupled receptors. Paradoxically, high-resolution structures are not available to facilitate rational drug design. Difficulties in expression, purification, and crystallization of these transmembrane receptors are the reasons for the low success rate. Recent individual and network-based technology development has significantly improved our knowledge of structural biology and might soon bring a major breakthrough in this area.
目前超过60%的药物是基于G蛋白偶联受体研发的。矛盾的是，尚无高分辨率结构可用于辅助合理药物设计。这些跨膜受体在表达、纯化和结晶方面存在困难，是成功率低的原因。最近基于个体和网络的技术发展显著增进了我们对结构生物学的认识，可能很快在这一领域带来重大突破。
