西亚试剂：Activity-Based Probe for Specific Photoaffinity Labeling γ-

Activity-Based Probe for Specific Photoaffinity Labeling γ-Aminobutyric Acid B (GABAB) Receptors on Living Cells: Design, Synthesis, and Biological Evaluation

Xin Li,‡§ Jian-Hua Cao,†§ Ying Li,†§ Philippe Rondard,# Yang Zhang,† Ping Yi,† Jian-Feng Liu,*† and Fa-Jun Nan*‡

Key Laboratory of Molecular Biophysics of Ministry of Education, School of Life Science and Technology, Huazhong University of Science and Technology, 1037 Luo Yu Road, Wuhan, Hubei, China, National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes of Biological Sciences, Chinese Academy of Sciences, 189 Guo Shou Jing Road, Shanghai 201203, China, and Institute of Functional Genomics, CNRS UMR5203, INSERM U661, University of Montpellier 1 and 2, Montpellier, F-34094, France

Abstract:

A trimodular activity-based probe was designed, synthesized, characterized, and applied to photoaffinity label the GABAB 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 GABAB receptors on living cells.

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