Li Xin, Cao Jian-Hua, Li Ying, Rondard Philippe, Zhang Yang, Yi Ping, Liu Jian-Feng, Nan Fa-Jun
Key Laboratory of Molecular Biophysics of Ministry of Education, School of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, Hubei, China.
J Med Chem. 2008 Jun 12;51(11):3057-60. doi: 10.1021/jm800140f. Epub 2008 May 1.
A trimodular activity-based probe was designed, synthesized, characterized, and applied to photoaffinity label the GABA(B) receptors transiently expressed in Chinese hamster ovary (CHO) cells. The probe exhibits specific binding activity at the ligand-binding pocket of GB1 subunits and high specificity of photoaffinity labeling, which makes the probe valuable for studying the localization and function of GABA(B) receptors on living cells.
设计、合成、表征了一种基于活性的三联体探针,并将其应用于光亲和标记瞬时表达于中国仓鼠卵巢(CHO)细胞中的γ-氨基丁酸B(GABA(B))受体。该探针在GB1亚基的配体结合口袋处表现出特异性结合活性以及高特异性的光亲和标记能力,这使得该探针对于研究活细胞上GABA(B)受体的定位和功能具有重要价值。