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GABA Receptor Oligomers' Structure and Function Discovered, Revealing Brain Function Role
GABA receptor oligomers exist in neurons and play an essential role in normal brain function, according to new research. The cryo-EM structure of a hetero-tetramer reveals how heterodimers interact asymmetrically to prevent activation of one unit.
G protein-coupled receptors (GPCRs) oligomerization may allow signal integration from different GPCR units. The GABA receptor, activated by the main inhibitory transmitter GABA, is an obligatory heterodimer and the target of two therapeutic drugs, baclofen and GHB. While GABA can form stable oligomers, the existence, roles, and possible allosteric interaction of GABA oligomers remain elusive. A new study published in *Nature Communications* reveals that GABA oligomers exist in neurons. According to the study, their function can be specifically affected by human disease-associated mutations, demonstrating their essential role in normal brain function. The study further reveals the cryo-EM structure of a hetero-tetramer in the apo state, which shows the heterodimers interacting in an asymmetrical way to prevent one unit from being activated.
Key Facts
- G protein-coupled receptors (GPCRs) oligomerization may allow signal integration from different GPCR units.
- The GABA receptor is activated by the main inhibitory transmitter, GABA.
- The GABA receptor is an obligatory heterodimer.
- The GABA receptor is the target of two therapeutic drugs, baclofen and GHB.
- GABA can form stable oligomers.
- GABA oligomers exist in neurons.
- The function of GABA oligomers can be specifically affected by human disease-associated mutations.
- The cryo-EM structure of a hetero-tetramer in the apo state reveals the heterodimers interacting in an asymmetrical way to prevent one unit from being activated.