Drugging the undruggable: gabapentin, pregabalin and the calcium channel α2δ subunit

2016 ◽  
Vol 51 (4) ◽  
pp. 246-256 ◽  
Author(s):  
James Offord ◽  
Lori L. Isom
Keyword(s):  
Calcium Channel ◽  
Α2δ Subunit

scholarly journals Molecular Diversity of the Calcium Channel α2δ Subunit

1999 ◽  
Vol 19 (2) ◽  
pp. 684-691 ◽  
Author(s):  
Norbert Klugbauer ◽  
Lubica Lacinová ◽  
Elsé Marais ◽  
Muriel Hobom ◽  
Franz Hofmann
Keyword(s):  
Calcium Channel ◽  
Molecular Diversity ◽  
Α2δ Subunit

scholarly journals Presynaptic CaV2 calcium channel traffic requires CALF-1 and the α2δ subunit UNC-36

2009 ◽  
Vol 12 (10) ◽  
pp. 1257-1265 ◽  
Author(s):  
Yasunori Saheki ◽  
Cornelia I Bargmann
Keyword(s):  
Calcium Channel ◽  
Α2δ Subunit

Investigation into the preferred conformation of gabapentin for interaction with its binding site on the α2δ subunit of a calcium channel

1997 ◽  
Vol 7 (19) ◽  
pp. 2481-2484 ◽  
Author(s):  
Justin S. Bryans ◽  
Natasha Davies ◽  
Nicolas S. Gee ◽  
David C. Horwell ◽  
Clare O. Kneen ◽  
...  
Keyword(s):  
Calcium Channel ◽  
Binding Site ◽  
Α2δ Subunit

scholarly journals straightjacket is required for the synaptic stabilization of cacophony, a voltage-gated calcium channel α1 subunit

2008 ◽  
Vol 181 (1) ◽  
pp. 157-170 ◽  
Author(s):  
Cindy V. Ly ◽  
Chi-Kuang Yao ◽  
Patrik Verstreken ◽  
Tomoko Ohyama ◽  
Hugo J. Bellen
Keyword(s):  
Calcium Channel ◽  
Neuronal Excitability ◽  
Neuromuscular Junctions ◽  
Synaptic Function ◽  
Voltage Gated ◽  
Α2δ Subunit ◽  
Voltage Gated Calcium Channel ◽  
Α1 Subunit ◽  
Synaptic Level ◽  
Synaptic Stabilization

In a screen to identify genes involved in synaptic function, we isolated mutations in Drosophila melanogaster straightjacket (stj), an α2δ subunit of the voltage-gated calcium channel. stj mutant photoreceptors develop normal synaptic connections but display reduced “on–off” transients in electroretinogram recordings, indicating a failure to evoke postsynaptic responses and, thus, a defect in neurotransmission. stj is expressed in neurons but excluded from glia. Mutants exhibit endogenous seizure-like activity, indicating altered neuronal excitability. However, at the synaptic level, stj larval neuromuscular junctions exhibit approximately fourfold reduction in synaptic release compared with controls stemming from a reduced release probability at these synapses. These defects likely stem from destabilization of Cacophony (Cac), the primary presynaptic α1 subunit in D. melanogaster. Interestingly, neuronal overexpression of cac partially rescues the viability and physiological defects in stj mutants, indicating a role for the α2δ Ca2+ channel subunit in mediating the proper localization of an α1 subunit at synapses.

(l)-Phenylglycine, but not necessarily other α2δ subunit voltage-gated calcium channel ligands, attenuates neuropathic pain in rats

Pain ◽  
2006 ◽  
Vol 125 (1) ◽  
pp. 136-142 ◽  
Author(s):  
James J. Lynch ◽  
Prisca Honore ◽  
David J. Anderson ◽  
William H. Bunnelle ◽  
Kathleen H. Mortell ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Calcium Channel ◽  
Voltage Gated ◽  
Α2δ Subunit ◽  
Voltage Gated Calcium Channel

A Calcium Channel from the Presynaptic Nerve Terminal of the Narke japonica Electric Organ Contains a Non-N-Type α2δ Subunit

2002 ◽  
Vol 65 (2) ◽  
pp. 831-836 ◽  
Author(s):  
Hiroshi Tokumaru ◽  
Suzuyo Shojaku ◽  
Hiroaki Takehara ◽  
Naohide Hirashima ◽  
Teruo Abe ◽  
...  
Keyword(s):  
Calcium Channel ◽  
Nerve Terminal ◽  
Electric Organ ◽  
Presynaptic Nerve Terminal ◽  
Α2δ Subunit

Identification of Novel Ligands for the Gabapentin Binding Site on the α2δ Subunit of a Calcium Channel and Their Evaluation as Anticonvulsant Agents

1998 ◽  
Vol 41 (11) ◽  
pp. 1838-1845 ◽  
Author(s):  
Justin S. Bryans ◽  
Natasha Davies ◽  
Nicolas S. Gee ◽  
Visaka U. K. Dissanayake ◽  
Giles S. Ratcliffe ◽  
...  
Keyword(s):  
Calcium Channel ◽  
Binding Site ◽  
Anticonvulsant Agents ◽  
Α2δ Subunit
Sign in / Sign up

Export Citation Format

Share Document