Activity-based probe for specific photoaffinity labeling gamma-aminobutyric acid B (GABAB) receptors on living cells: design, synthesis, and biological evaluation.
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.
Li
Xin
X
Key Laboratory of Molecular Biophysics of Ministry of Education, School of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, Hubei, China.
Cao
Jian-Hua
JH
Li
Ying
Y
Rondard
Philippe
P
Zhang
Yang
Y
Yi
Ping
P
Liu
Jian-Feng
JF
Nan
Fa-Jun
FJ
D000818:Animals; D001565:Benzoates / Q000138:chemical synthesis* / Q000378:metabolism; D001896:Boron Compounds / Q000138:chemical synthesis* / Q000378:metabolism; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D003978:Diazomethane / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D009943:Organophosphorus Compounds / Q000138:chemical synthesis / Q000378:metabolism; D019920:Photoaffinity Labels / Q000138:chemical synthesis* / Q000378:metabolism; D021122:Protein Subunits / Q000378:metabolism; D018080:Receptors, GABA-B / Q000378:metabolism*; D013329:Structure-Activity Relationship
C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001565:Benzoates; D001896:Boron Compounds; D009943:Organophosphorus Compounds; D019920:Photoaffinity Labels; D021122:Protein Subunits; D018080:Receptors, GABA-B; D003978:Diazomethane