Prospects for Rational Development of Pharmacological Gap Junction Channel Blockers

2002 ◽  
Vol 3 (6) ◽  
pp. 455-464 ◽  
Author(s):  
Bentham Science Publisher David C. Spray ◽  
Bentham Science Publisher Renato Rozental ◽  
Bentham Science Publisher Miduturu Srinivas
Keyword(s):  
Gap Junction ◽  
Channel Blockers ◽  
Rational Development ◽  
Gap Junction Channel

Neuroprotection in the treatment of glaucoma – A focus on connexin43 gap junction channel blockers

2015 ◽  
Vol 95 ◽  
pp. 182-193 ◽  
Author(s):  
Ying-Shan Chen ◽  
Colin R. Green ◽  
Helen V. Danesh-Meyer ◽  
Ilva D. Rupenthal
Keyword(s):  
Gap Junction ◽  
Channel Blockers ◽  
Gap Junction Channel

scholarly journals New Classes of Gap Junction Channel Blockers for Cx43 and Cx50

2010 ◽  
Vol 98 (3) ◽  
pp. 94a
Author(s):  
Silke B. Bodendiek ◽  
Clio Rubinos ◽  
Miduturu Srinivas ◽  
Heike Wulff
Keyword(s):  
Gap Junction ◽  
Channel Blockers ◽  
Gap Junction Channel

scholarly journals The potential antiepileptogenic effect of neuronal Cx36 gap junction channel blockage

2021 ◽  
Vol 12 (1) ◽  
pp. 46-51
Author(s):  
Guangliang Wang ◽  
Xuemei Wu
Keyword(s):  
Gap Junction ◽  
Neuronal Injury ◽  
Channel Blockers ◽  
Gap Junction Channels ◽  
New Antiepileptic Drugs ◽  
Gap Junction Channel ◽  
Promising Strategy ◽  
Patients With Epilepsy

Abstract Epilepsy is one of the most prevalent neurological disorders and can result in neuronal injury and degeneration. Consequently, research into new antiepileptic drugs capable of providing protection against neuronal injury and degeneration is extremely important. Neuronal Cx36 gap junction channels have been found to play an important role in epilepsy; thus, pharmacological interference using Cx36 gap junction channel blockers may be a promising strategy for disrupting the synchronization of neurons during seizure activity and protecting neurons. Based on these promising findings, several in vivo and in vitro studies are ongoing and the first encouraging results have been published. The results bring hope that neurons can be protected from injury and degeneration in patients with epilepsy, which is currently impossible.

scholarly journals Cholesterol modulates function of connexin 43 gap junction channel via PKC pathway in H9c2 cells

2014 ◽  
Vol 1838 (8) ◽  
pp. 2019-2025 ◽  
Author(s):  
Jun Zou ◽  
Xiao-Yang Yue ◽  
Sheng-Chao Zheng ◽  
Guangwei Zhang ◽  
He Chang ◽  
...  
Keyword(s):  
Gap Junction ◽  
Connexin 43 ◽  
H9c2 Cells ◽  
Gap Junction Channel

A Closed Gap Junction Channel State Caused By A Single Site Mutation in the 3rd Transmembrane Helix

2004 ◽  
Vol 10 (S02) ◽  
pp. 1498-1499 ◽  
Author(s):  
Derek L Beahm ◽  
Guido Gaietta ◽  
Anjana Chandrasekhar ◽  
Galen M Hand ◽  
Amy Smock ◽  
...  
Keyword(s):  
Gap Junction ◽  
Transmembrane Helix ◽  
Single Site ◽  
Site Mutation ◽  
Channel State ◽  
Gap Junction Channel

Extended abstract of a paper presented at Microscopy and Microanalysis 2004 in Savannah, Georgia, USA, August 1–5, 2004.

scholarly journals Identification of amino acid residues lining the pore of a gap junction channel

2002 ◽  
Vol 159 (2) ◽  
pp. 349-360 ◽  
Author(s):  
I.M. Skerrett ◽  
J. Aronowitz ◽  
J.H. Shin ◽  
G. Cymes ◽  
E. Kasperek ◽  
...  
Keyword(s):  
Gap Junction ◽  
Molecular Level ◽  
Close Association ◽  
Pore Wall ◽  
Van Der Waals Interactions ◽  
Amino Acid Residues ◽  
Fixed Charges ◽  
Gap Junction Channel ◽  
Multicellular Organisms ◽  
Pore Lining

Gap junctions represent a ubiquitous and integral part of multicellular organisms, providing the only conduit for direct exchange of nutrients, messengers and ions between neighboring cells. However, at the molecular level we have limited knowledge of their endogenous permeants and selectivity features. By probing the accessibility of systematically substituted cysteine residues to thiol blockers (a technique called SCAM), we have identified the pore-lining residues of a gap junction channel composed of Cx32. Analysis of 45 sites in perfused Xenopus oocyte pairs defined M3 as the major pore-lining helix, with M2 (open state) or M1 (closed state) also contributing to the wider cytoplasmic opening of the channel. Additional mapping of a close association between M3 and M4 allowed the helices of the low resolution map (Unger et al., 1999. Science. 283:1176–1180) to be tentatively assigned to the connexin transmembrane domains. Contrary to previous conceptions of the gap junction channel, the residues lining the pore are largely hydrophobic. This indicates that the selective permeabilities of this unique channel class may result from novel mechanisms, including complex van der Waals interactions of permeants with the pore wall, rather than mechanisms involving fixed charges or chelation chemistry as reported for other ion channels.

Innexin-3 forms connexin-like intercellular channels

1999 ◽  
Vol 112 (14) ◽  
pp. 2391-2396 ◽  
Author(s):  
Y. Landesman ◽  
T.W. White ◽  
T.A. Starich ◽  
J.E. Shaw ◽  
D.A. Goodenough ◽  
...  
Keyword(s):  
Caenorhabditis Elegans ◽  
Gap Junction ◽  
Functional Properties ◽  
Xenopus Oocytes ◽  
Family Members ◽  
Electrical Coupling ◽  
Large Family ◽  
Gap Junction Channel ◽  
Intercellular Channels

Innexins comprise a large family of genes that are believed to encode invertebrate gap junction channel-forming proteins. However, only two Drosophila innexins have been directly tested for the ability to form intercellular channels and only one of those was active. Here we tested the ability of Caenorhabditis elegans family members INX-3 and EAT-5 to form intercellular channels between paired Xenopus oocytes. We show that expression of INX-3 but not EAT-5, induces electrical coupling between the oocyte pairs. In addition, analysis of INX-3 voltage and pH gating reveals a striking degree of conservation in the functional properties of connexin and innnexin channels. These data strongly support the idea that innexin genes encode intercellular channels.

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