Description
2GBI (5418-95-1) is a selective and state-dependent blocker of voltage-gated proton channels (Hv1).12GBI blocks the channel by binding to the voltage-sensing domain from its intracellular side.2,3 Inhibition of Hv1 is a potentially new target of intervention in various pathophysiological processes including inflammatory, cancer, bone resorption and neurodegenerative disease.4
References
[1] LIANG HONG. Interrogation of the intersubunit interface of the open Hv1 proton channel with a probe of allosteric coupling.[J]. Scientific Reports, 2015: 14077. DOI:
10.1038/srep14077[2] LIANG HONG Francesco T Iris H Kim. Molecular determinants of Hv1 proton channel inhibition by guanidine derivatives.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2014: 9971-9976. DOI:
10.1073/pnas.1324012111[3] ELEONORA GIANTI. On the role of water density fluctuations in the inhibition of a proton channel.[J]. Journal of Family Violence, 2016, 3 1: E8359-E8368. DOI:
10.1073/pnas.1609964114[4] AMAURY PUPO Carlos G L. In pursuit of an inhibitory drug for the proton channel.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2014: 9673-9674. DOI:
10.1073/pnas.1408808111
