The structural biologist was the first to solve the crystal structures of two different artemisinin derivatives artesunate and artemether in a complex with gephyrin
. By binding to inhibitory glycine and GABAA receptors, gephyrin
acts as a central scaffold protein of inhibitory postsynapses in the mammalian central nervous system.
Consistent with this computational prediction, immunohistological analyses revealed significantly decreased numbers of [GABA.sub.A] receptor and gephyrin
clusters in the granule cell layer of NL2 KOs, indicating a loss of synaptic [GABA.sub.A] receptors from the somata of granule cells.
is a major scaffolding molecule of inhibitory postsynaptic specialization.
Very recently, long-term treatment with antimalarial drugs that target gephyrin
(a protein that participates in GABAA-R transport to the membrane), or treatment with GABA, was shown to promote islet [alpha]-cell transdifferentiation into [beta]-cells [22, 23].
In transgenic (TG2576) and Swedish transgenic (TG-SwDI) mice, dihydromyricetin may reduce A[beta] peptide production and restore gephyrin
levels, GABAergic transmission, and functional synapses, leading to improvement of clinical symptoms .
Burkarth N, Kriebel M, Kranz EU, Volkmer H, 2007, Neurofascin regulates the formation of gephyrin
clusters and their subsequent translocation to the axon hillock of hippocampal neurons.
Splice-specific Functions of Gephyrin
in Molybdenum Cofactor Biosynthesis, Journal of Biological Chemistry 283 (25): 17370-9.
 Antibodies directed against gephyrin
, a post-synaptic cytosolic vesicle protein, may also be produced.
Bechade, "Expression of glycine receptor a subunits and gephyrin
in cultured spinal neurons," European Journal of Neuroscience, vol.
 A study by Chhatwal and colleagues,  found that gephyrin
(which regulates GABAergic neurotransmission by clustering GABAA receptors at the synapse) is unregulated after extinction training but down-regulated after fear acquisition, confirming the role of GABAA receptors in both fear acquisition and extinction.
Fast and reversible trapping of surface glycine receptors by gephyrin
. Nat Neurosci 2001;4:253-60.
A major inhibitory synaptic receptor is the hetero-pentameric GABAA Receptor (GABAAR), which is stabilised in the synapse by the intracellular scaffolding protein gephyrin
, in turn, is recruited to and stabilised at the synapse by the adhesion protein neuroligin-2 (NL2).