[HTML][HTML] 5-Chloro-2-Guanidinobenzimidazole (ClGBI) Is a Non-Selective Inhibitor of the Human HV1 Channel
5-chloro-2-guanidinobenzimidazole (ClGBI), a small-molecule guanidine derivative, is a
known effective inhibitor of the voltage-gated proton (H+) channel (HV1, Kd≈ 26 μM) and is …
known effective inhibitor of the voltage-gated proton (H+) channel (HV1, Kd≈ 26 μM) and is …
Introducing NZ-58, a potent inhibitor of the human voltage-gated proton channel
Á Fehér, É Korpos, K Gyuris, G Domingos, M Piga… - Biophysical …, 2024 - cell.com
The human voltage-gated proton channel (hH V 1) has a main role in the regulation of
intracellular pH, preventing acidosis. Furthermore, hH V 1 has been shown to play role in the …
intracellular pH, preventing acidosis. Furthermore, hH V 1 has been shown to play role in the …
Molecular determinants of Hv1 proton channel inhibition by guanidine derivatives
The voltage-gated proton channel Hv1 plays important roles in proton extrusion, pH
homeostasis, and production of reactive oxygen species in a variety of cell types. Excessive …
homeostasis, and production of reactive oxygen species in a variety of cell types. Excessive …
[HTML][HTML] Discovery and validation of new Hv1 proton channel inhibitors with onco-therapeutic potential
A El Chemaly, V Jaquet, Y Cambet, A Caillon… - … et Biophysica Acta (BBA …, 2023 - Elsevier
The voltage-gated hydrogen channel Hv1 encoded in humans by the HVCN1 gene is a
highly selective proton channel that allows large fluxes of protons across biological …
highly selective proton channel that allows large fluxes of protons across biological …
HIFs: New arginine mimic inhibitors of the Hv1 channel with improved VSD–ligand interactions
The human voltage-gated proton channel Hv1 is a drug target for cancer, ischemic stroke,
and neuroinflammation. It resides on the plasma membrane and endocytic compartments of …
and neuroinflammation. It resides on the plasma membrane and endocytic compartments of …
Cell glycosaminoglycans content modulates human voltage‐gated proton channel (HV1) gating
DJB Orts, M Arcisio‐Miranda - The FEBS Journal, 2022 - Wiley Online Library
Voltage‐gated proton channels (HV1) have been found in many mammalian cells and play
a crucial role in the immune system, male fertility, and cancer progression …
a crucial role in the immune system, male fertility, and cancer progression …
Identification of a Novel Structural Class of HV1 Inhibitors by Structure-Based Virtual Screening
M Piga, Z Varga, A Feher, F Papp… - Journal of Chemical …, 2024 - ACS Publications
The human voltage-gated proton channel, hHV1, is highly expressed in various cell types
including macrophages, B lymphocytes, microglia, sperm cells and also in various cancer …
including macrophages, B lymphocytes, microglia, sperm cells and also in various cancer …
The HCN channel as a pharmacological target: Why, where, and how to block it
Hyperpolarization-activated, cyclic nucleotide-gated (HCN) channels, expressed in a variety
of cell types and in all tissues, control excitation and rhythm. Since their discovery in neurons …
of cell types and in all tissues, control excitation and rhythm. Since their discovery in neurons …
In pursuit of an inhibitory drug for the proton channel
A Pupo, C Gonzalez León - Proceedings of the National …, 2014 - National Acad Sciences
Of the∼ 22,000 protein-coding genes in the human genome, an estimated 8,000 are
druggable (1). The current drug market targets no more than 450 unique human proteins (1) …
druggable (1). The current drug market targets no more than 450 unique human proteins (1) …
Voltage-Gated Proton Channels: Molecular Biology, Physiology, and Pathophysiology of the HV Family
TE DeCoursey - Physiological reviews, 2013 - journals.physiology.org
Voltage-gated proton channels (HV) are unique, in part because the ion they conduct is
unique. HV channels are perfectly selective for protons and have a very small unitary …
unique. HV channels are perfectly selective for protons and have a very small unitary …