Potent, State-Independent, and Specific Inhibitor of the Human Proton Channel Hv1

Tech ID: 30417 / UC Case 2019-915-0

Brief Description

Researchers at UCI have engineered a class of Hv1 polypeptide modulators that selectively modulate Hv1 voltage gated channels while leaving other voltage gated channels unaffected. With no Hv1 modulators currently on the market, this class of Hv1 polypeptide modulators could provide solutions in birth control, autoimmune therapies, tumor reduction, and inflammatory disease treatment.

Suggested uses

  • Inflammatory Diseases – Inhibit inflammatory response in Acute Lung Injury/ARDS, stroke, neurodegeneration, and both neuropathic and inflammatory pain
  • Birth Control – Inhibition of sperm maturation
  • Autoimmune Therapies – Reducing reactive oxygen species (ROS) in white blood cells
  • Cancer Therapeutics – Tumor reduction


·Polypeptides selectively target only Hv1 voltage gated channels

·Includes both reversible and irreversible modulators

·Cell type specific response

·Monomeric peptide is effective at inhibiting ROS production in white blood cells and sperm capacitation in μM range

·Dimeric peptide can block the Hv1 channel in both open and closed states with picomolar affinity

Full Description

Cells use voltage gated channels to create gradients which are used for important cellular functions. The ability to modulate these voltage gated channels allows for control of important cellular functions. The Hv1 voltage gated channel is an attractive therapeutic target due to its high expression in some metastatic cancers, its role in sperm maturation, and its use by white blood cells to produce reactive oxygen species for inflammatory responses. Currently no selective Hv1 channel inhibitors are on the market.

Researchers at UCI have developed a class of polypeptides that act as selective Hv1 channel modulators. These polypeptides can reversibly or irreversibly inhibit the Hv1 channel. The unique structure of the modulators allows them to selectively target the Hv1 channel while leaving other voltage gated channels unaffected. The polypeptide modulators also have their amino acid sequence tailored to fine-tune the channel inhibition. Preliminary results for the monomeric peptide have shown efficacy for limiting ROS production and sperm maturation at µM concentrations. The newly developed dimeric peptide is more potent than the monomeric form – it blocks the channel in both open and closed states with picomolar affinity. The UCI Hv1 polypeptide modulator shows promise for applications in birth control, autoimmune therapy, and cancer.

State Of Development

Dimeric peptide was validated in vitro on the Hv1 channel to show inhibition of function and picomolar effectiveness.Additional in vitro and in vivo studies are currently in progress to further assess the activities of both the monomeric and dimeric peptides.

Patent Status

Country Type Number Dated Case
United States Of America Issued Patent 11,274,130 03/15/2022 2019-915
United States Of America Published Application 2022028980 09/15/2022 2019-915

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  • Goldstein, Steven A.N.

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